Factory direct sales, accept customization. Lifitegrast is API for the treatment of signs and symptoms of dry eye, a syndrome called keratoconjunctivitis sicca. Kind Pharma has its own laboratory, we can do analytical testing for API (Active Pharma
Cas:1025967-78-5
Min.Order:1 Kilogram
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Type:Lab/Research institutions
inquiryBoiling Point:811.9±65.0 °C(Predicted) PKA:3.14±0.10(Predicted) PSA:142.37000 Density:1.479±0.06 g/cm3(Predicted) LogP:6.17690 Storage Temp.:Hygroscopic, -20°C Freezer, Under inert atmosphere Solubility.:DMS
Cas:1025967-78-5
Min.Order:1 Gram
FOB Price: $2.0 / 5.0
Type:Trading Company
inquiryJinlan Pharm-Drugs Technology Co.,Limited (with its export company Hangzhou Royall Import & Export Co.,Ltd.)is located in Hangzhou, Zhejiang Province. Neighboring Ningbo port, Shanghai port, Hangzhou Xiaoshan Int’l Airport and Shanghai Pu
KONING PHARMCHEM CO., LTD. has committed itself to a strategy of providing a unique service for companies involved in the manufacture of pharmaceuticals, healthcare products, food, cosmetics and other fine chemicals. Our products including but not li
Unique advantages of Lifitegrast Cas 1025967-78-5 Guaranteed purity High quality & competitive price Quality control Fast feedback Prompt shipment Appearance:White powder Storage:cool dry place Package:1kg/foil bag;25kg/drum Application:med
Cas:1025967-78-5
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Type:Trading Company
inquiryLifitegrast CAS No.:1025967-78-5 Name: Lifitegrast Synonyms: N-[[2-(6-Benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-L-phenylalanine; SAR 1118
Cas:1025967-78-5
Min.Order:1 Kilogram
FOB Price: $2.0
Type:Other
inquiryOur main production base is located in Xuzhou industry park. We are certified both to the ISO 9001 and ISO 14001 Standards, have a safety management system in place.Our R&D team masters core technology for process-design of target building block
WITH US,YOUR MONEY IN SAFE,YOUR BUSINESS IN SAFE 1)Quick Response Within 12 hours; 2)Quality Guarantee: All products are strictly tested by our QC, confirmed by QA and approved by third party lab in China, USA, Canada, Germany, UK, Italy, France et
Cas:1025967-78-5
Min.Order:10 Gram
FOB Price: $146.0 / 176.0
Type:Trading Company
inquiryProduct Name Lifitegrast Alias ifitegrast;CS-2633;Lifitegrast(API);SAR-1118;SAR1118;Lifitegrast-d4;Lifitegrast Impurity;lifitegrast;Lifitegrast, SAR 1118 CAS No. 1025967-78-5 Molecular Formula C29H2
Cas:1025967-78-5
Min.Order:1 Kilogram
FOB Price: $1.0
Type:Other
inquiryWith our good experience, we offer detailed technical support and advice to assist customers. We communicate closely with customers to establish their quality requirements. Consistent Quality Our plant has strict quality control in each manufactu
Cas:1025967-78-5
Min.Order:1 Kilogram
FOB Price: $1.0 / 10.0
Type:Trading Company
inquiryWuhan hanweishi Pharmchem Co., Ltd(Hanways chempharm) is a specialized company concentrating on the R&D, production, marketing and technical service of APIs and pharmaceutical intermediates. The leading products range are APIs, Hormones, Peptides
Cas:1025967-78-5
Min.Order:100 Kilogram
FOB Price: $1.0 / 5.0
Type:Trading Company
inquirylifitegrast Chemical Properties Boiling point 811.9±65.0 °C(Predicted) density 1.479±0.06 g/cm3(Predicted) pka 3.14±0.10(Predicted) lifitegrast Chemical Properties Boiling point 811.9±65.0 °C(Predi
lifitegrast CAS: 1025967-78-5 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of chemical intermediates, specializing in high quality organic intermedia
Cas:1025967-78-5
Min.Order:1 Gram
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Type:Lab/Research institutions
inquiryHello, dear friend! I'm Hansen and Allen from China. Welcome to my lookchem mall! The following is a brief introduction of our company's products and services. If you are interested in our products, please contact us by emai
Henan Wentao Chemical Product Co.,Ltd is Located in Zhengzhou High-tech Development Zone with import and export license, We passed ISO 9001:2008 as well, Henan Wentao has developed more than 1000 compounds, which are widely used in the fields of prod
Our Advantage: high quality with competitive price High quality standard: BP/USP/EP Enterprise standard All purity customized Fast and safe delivery We have reliable forwarder who can help us deliver our goods more fast and safe. We
Cas:1025967-78-5
Min.Order:10 Kilogram
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Type:Trading Company
inquiryHubei Yuanmeng Biological Technology Co., Ltd., which is located in Wuhan, China. We are specializing in the exportation of APIs, and plant extracts ect. Our products has been exported to America, Australia, Brazil, the Europe, Middle East and other
Cas:1025967-78-5
Min.Order:1 Kilogram
FOB Price: $3.0 / 5.0
Type:Trading Company
inquiryOur company provides one-stop services of research - development - production for a variety of special prouducts. Not only do we make effective use of our strong technological strength, but also establish of cooperative relations with several well-
Cas:1025967-78-5
Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryCompany Introduction 1. Established in 2005, with two independent business divisions: Fine chemicals division; Pharmaceutical division. 2. Main product: Optical brightener Textile auxiliary Dye stuff Pigments
J&H CHEM R&D center can offer custom synthesis according to the contract research and development services for the fine chemicals, pharmaceutical, biotechnique and some of the other chemicals. J&H CHEM has some Manufacturing base in Jia
Our Advantages Production: Advanced chemical equipment with years of experience.Staffs for producing various extract products. Quality Control:A complete set of Testing Professional and Analysis Equipment ensures the Quality Requirements and Speci
Cas:1025967-78-5
Min.Order:1 Kilogram
FOB Price: $150.0 / 180.0
Type:Trading Company
inquiryZibo Hangyu Biotechnology Development Co., Ltd is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemi
Cas:1025967-78-5
Min.Order:10 Gram
FOB Price: $100.0
Type:Lab/Research institutions
inquiryWe are one of a few suppliers that can offer custom synthesis service of this product We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research. We are committed to prov
Cas:1025967-78-5
Min.Order:100 Gram
FOB Price: $100.0 / 2000.0
Type:Lab/Research institutions
inquiryChemvon Biotechnology Co. Ltd., established in the end of 2004, is a high-technology pharmaceutical and fine chemical company in R&D, manufacturing and sales of Lifitegrast . With the experience and specialization in technology of asymmetric sy
Why is SINOWAY: 1) Specialized in pharmaceutical and healthcare industrial for 34 years. 2) ISO 9001:2015 & SGS audited supplier . 3) Accept various payment terms : T.T 30-60 days. 4) We have warehouse in USA with quickly shipment . 5) We c
Cas:1025967-78-5
Min.Order:1 Kilogram
Negotiable
Type:Trading Company
inquiryOur company was built in 2009 with an ISO certificate.In the past 6 years, we have grown up as a famous fine chemicals supplier in China and we had established stable business relationships with Samsung,LG,Merck,Thermo Fisher Scientific and so on.O
Cas:1025967-78-5
Min.Order:1 Kilogram
FOB Price: $1000.0
Type:Lab/Research institutions
inquiryProduct name: Lifitegrast CAS No.:1025967-78-5 Molecule Formula:C29H24Cl2N2O7S Molecule Weight:615.48 Purity: 99.0% Package: 25kg/drum Description:White powder Manufacture Standards:Enterprise Standard TESTING ITEMS
Cas:1025967-78-5
Min.Order:1 Kilogram
Negotiable
Type:Lab/Research institutions
inquiryProduct Details Grade: pharmaceutical grade Purity:99%+ ProductionCapacity: 1000 Kilogram/Month Scope of use: For scientific research only(The product must be used legally) Our Advantage 1. Best quality with competitive price. 2. Quick shipping,
Cas:1025967-78-5
Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryGMP standard, high purity, competitive price, in stock 1. Quick Response: within 6 hours after receiving your email. 2. Quality Guarantee: All products are strictly tested by our QC, confirmed by QA, and approved by a third-party lab in China, USA,
factory?direct?saleAppearance:White Powder Storage:Store In Dry, Cool And Ventilated Place Package:25kg/drum, also according to the clients requirement Application:It is widely used as a thickener, emulsifier and stabilizer Transportation:By Sea Or B
Cas:1025967-78-5
Min.Order:1 Kilogram
FOB Price: $18.0 / 20.0
Type:Trading Company
inquiry(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With phosphoric acid In dichloromethane; water at 50℃; for 0.5h; | 96% |
((S)-benzyl 2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-methylsulfonyl)phenyl)propanoate
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With formic acid; palladium 10% on activated carbon; triethylamine In tetrahydrofuran; methanol at 20℃; for 4h; | 95% |
With formic acid; palladium 10% on activated carbon; triethylamine In tetrahydrofuran; methanol Reagent/catalyst; Solvent; | n/a |
With lithium hydroxide monohydrate In water; acetone at -5 - 0℃; for 1h; Reagent/catalyst; Solvent; Temperature; | |
With hydrogenchloride In water; acetonitrile at 3 - 25℃; for 19.5h; Solvent; Temperature; Reagent/catalyst; Inert atmosphere; | 3.8 g |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Stage #1: 2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3 ,4-tetrahydroisoquinoline-6-carboxylic acid With [2-(1H-indol-3-yl)-ethyl]-methylamine; N-ethyl-N,N-diisopropylamine; HATU In tetrahydrofuran at 40℃; for 2h; Inert atmosphere; Stage #2: (S)-2-amino-3-(3-(methylsulfonyl)phenyl)propanoic acid In tetrahydrofuran at 20 - 30℃; | 92% |
Stage #1: 2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3 ,4-tetrahydroisoquinoline-6-carboxylic acid With triethylamine In N,N-dimethyl-formamide at 28℃; for 0.166667h; Stage #2: With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 5 - 8℃; for 2h; Stage #3: (S)-2-amino-3-(3-(methylsulfonyl)phenyl)propanoic acid In N,N-dimethyl-formamide at 8℃; for 1h; |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-amino-3-(3-(methylsulfonyl)phenyl)propanoic acid; 3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl 2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxylate With N-ethyl-N,N-diisopropylamine In acetonitrile at 40 - 45℃; Stage #2: With hydrogenchloride In water at 0 - 5℃; for 1h; pH=5; | 87% |
With N-ethyl-N,N-diisopropylamine In water; acetonitrile at 20 - 45℃; for 4h; |
benzofuran-6-carboxylic acid
(S)-2-(5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at -10 - 20℃; Reagent/catalyst; Solvent; Temperature; | 83.8% |
With triethylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 10 - 20℃; for 1.5h; |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With water; lithium hydroxide In methanol at 25 - 30℃; for 3h; Reagent/catalyst; Solvent; | 80% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-amino-3-(3-(methylsulphonyl)phenyl)propanoic acid hydrochloride With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; Inert atmosphere; Stage #2: C19H12Cl3NO3 In dichloromethane at 0 - 5℃; Temperature; Inert atmosphere; | 77% |
(2S)-3-(3-bromophenyl)-2-[(tert-butoxycarbonyl)amino]propanoic acid
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: copper(l) iodide; caesium carbonate; L-proline / dimethyl sulfoxide / 9 h / 100 °C 2: dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / N,N-dimethyl-formamide / 20 °C 3: hydrogenchloride / 1,4-dioxane; dichloromethane; water / 0 °C 4: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 5: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 6: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 7: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 7 steps 1.1: copper(l) iodide; caesium carbonate; L-proline; sodium methansulfinate / dimethyl sulfoxide / 9 h / 95 - 100 °C 2.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap 3.1: hydrogenchloride / dichloromethane; 1,4-dioxane / 0 °C 4.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 4.2: 18 h / 20 °C 5.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 6.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 7.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 7 steps 1: copper(l) iodide; caesium carbonate; L-proline; sodium methansulfinate / dimethyl sulfoxide / 9 h / 95 - 100 °C 2: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap 3: hydrogenchloride / dichloromethane; 1,4-dioxane / 0 °C 4: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 5: hydrogenchloride / water; 1,4-dioxane 6: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 7: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
(S)-2-((tert-butoxycarbonyl)amino)-3-((3-methylsulfonyl)phenyl)propanol
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / N,N-dimethyl-formamide / 20 °C 2: hydrogenchloride / 1,4-dioxane; dichloromethane; water / 0 °C 3: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 4: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 5: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 6: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap 2.1: hydrogenchloride / dichloromethane; 1,4-dioxane / 0 °C 3.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 3.2: 18 h / 20 °C 4.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 5.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 6.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 6 steps 1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap 2: hydrogenchloride / dichloromethane; 1,4-dioxane / 0 °C 3: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 4: hydrogenchloride / water; 1,4-dioxane 5: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 6: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 6 steps 1.1: O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / dichloromethane / 0.25 h / 25 - 35 °C 1.2: 5 h / 25 - 45 °C 2.1: hydrogenchloride / 1,4-dioxane; dichloromethane / 2 h / 25 - 35 °C 3.1: triethylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate / N,N-dimethyl-formamide / 0.25 h / 25 - 35 °C 3.2: 5 h / 25 - 45 °C 4.1: hydrogenchloride / 1,4-dioxane; dichloromethane / 25 - 35 °C 5.1: triethylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate / N,N-dimethyl-formamide / 0.25 h / 25 - 35 °C 5.2: 5 h / 25 - 45 °C 6.1: lithium hydroxide monohydrate / tetrahydrofuran; water / 25 - 35 °C View Scheme |
(S)-benzyl 2-((tert-butoxycarbonyl)amino)-3-((3-methylsulfonyl)phenyl)propionate
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: hydrogenchloride / 1,4-dioxane; dichloromethane; water / 0 °C 2: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 3: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 4: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 5: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: hydrogenchloride / dichloromethane; 1,4-dioxane / 0 °C 2.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 2.2: 18 h / 20 °C 3.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 4.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 5.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 5 steps 1: hydrogenchloride / dichloromethane; 1,4-dioxane / 0 °C 2: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 3: hydrogenchloride / water; 1,4-dioxane 4: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 5: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
(2S)-2-amino-3-(3-(methanesulfonyl)phenyl)propionic acid benzyl ester hydrochloride
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 2: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 3: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 4: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 1.2: 18 h / 20 °C 2.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 4.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 4 steps 1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 2: hydrogenchloride / water; 1,4-dioxane 3: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 4: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
N-(2-chloroethyl)-3,5-dichlorobenzylamine hydrochloride
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1.1: aluminum (III) chloride / 185 °C 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 4 h / 20 °C 3.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine / tetrahydrofuran / -78 - 20 °C 3.2: -78 - 20 °C 4.1: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 5.1: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 6.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 7.1: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 7 steps 1.1: aluminum (III) chloride; ammonium chloride / 185 °C 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 3.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 4.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 4.2: 18 h / 20 °C 5.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 6.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 7.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 9 steps 1: aluminum (III) chloride; ammonium chloride / 185 °C 2: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 3: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 4: hydrogenchloride / 1,4-dioxane 5: sodium hydrogencarbonate 6: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 7: hydrogenchloride / water; 1,4-dioxane 8: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 9: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
C28H23Cl2N
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine / tetrahydrofuran / -78 - 20 °C 1.2: -78 - 20 °C 2.1: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 3.1: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 4.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 5.1: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 2.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 2.2: 18 h / 20 °C 3.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 4.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 5.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 7 steps 1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 2: hydrogenchloride / 1,4-dioxane 3: sodium hydrogencarbonate 4: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 5: hydrogenchloride / water; 1,4-dioxane 6: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 7: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
5,7-dichloro-2-trityl-1,2,3,4-tetrahydroisoquinoline-6-carboxylic acid
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 2: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 3: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 4: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 1.2: 18 h / 20 °C 2.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 4.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 6 steps 1: hydrogenchloride / 1,4-dioxane 2: sodium hydrogencarbonate 3: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 4: hydrogenchloride / water; 1,4-dioxane 5: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 6: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 3 steps 1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 20 h / 28 °C 2: sodium hydroxide / 1,4-dioxane; water / 2 h / 28 °C 3: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 1.5 h / 10 - 20 °C View Scheme |
C46H40Cl2N2O5S
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 2: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 3: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 2: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 3: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 2 steps 1: sodium hydroxide / 1,4-dioxane; water / 2 h / 28 °C 2: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 1.5 h / 10 - 20 °C View Scheme |
benzyl (S)-2-(5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-[3-(methylsulfonyl)phenyl]propanoate hydrochloride
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 2: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme |
3,5-dichlorobenzaldehyde
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1.1: methanol; sodium cyanoborohydride / 20 °C 2.1: aluminum (III) chloride / 185 °C 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 4 h / 20 °C 4.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine / tetrahydrofuran / -78 - 20 °C 4.2: -78 - 20 °C 5.1: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 6.1: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 7.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 8.1: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 10 steps 1: sodium cyanoborohydride 2: aluminum (III) chloride; ammonium chloride / 185 °C 3: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 4: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 5: hydrogenchloride / 1,4-dioxane 6: sodium hydrogencarbonate 7: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 8: hydrogenchloride / water; 1,4-dioxane 9: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 10: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 11 steps 1.1: ethanol / 2 h / 20 - 78 °C 2.1: sulfuric acid / dichloromethane / 7 h / 120 - 125 °C 2.2: 5 h / 0 - 50 °C / pH 12 3.1: platinum(IV) oxide / methanol / 0.17 h / 20 °C / Inert atmosphere 3.2: 25 h / 20 °C / 6464.52 Torr / Inert atmosphere 3.3: 0 - 40 °C 4.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 5.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 6.1: hydrogenchloride / 1,4-dioxane 7.1: sodium hydrogencarbonate 8.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 9.1: hydrogenchloride / water; 1,4-dioxane 10.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 11.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 8 steps 1.1: sodium cyanoborohydride 2.1: aluminum (III) chloride; ammonium chloride / 185 °C 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 4.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 5.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 5.2: 18 h / 20 °C 6.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 7.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 8.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 9 steps 1.1: ethanol / 2 h / 20 - 78 °C 2.1: sulfuric acid / dichloromethane / 7 h / 120 - 125 °C 2.2: 5 h / 0 - 50 °C / pH 12 3.1: platinum(IV) oxide / methanol / 0.17 h / 20 °C / Inert atmosphere 3.2: 25 h / 20 °C / 6464.52 Torr / Inert atmosphere 3.3: 0 - 40 °C 4.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 5.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 6.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 6.2: 18 h / 20 °C 7.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 8.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 9.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
5,7-dichloro-1,2,3,4-tetrahydroisoquinoline
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 4 h / 20 °C 2.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine / tetrahydrofuran / -78 - 20 °C 2.2: -78 - 20 °C 3.1: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 4.1: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 5.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 6.1: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 2.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 3.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 3.2: 18 h / 20 °C 4.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 5.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 6.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 8 steps 1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 2: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 3: hydrogenchloride / 1,4-dioxane 4: sodium hydrogencarbonate 5: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 6: hydrogenchloride / water; 1,4-dioxane 7: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 8: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
(S)-2-amino-3-(3-bromophenyl)propanoic acid
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1: sodium hydrogencarbonate / 1,4-dioxane; water / 20 °C 2: copper(l) iodide; caesium carbonate; L-proline / dimethyl sulfoxide / 9 h / 100 °C 3: dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / N,N-dimethyl-formamide / 20 °C 4: hydrogenchloride / 1,4-dioxane; dichloromethane; water / 0 °C 5: triethylamine; HATU / N,N-dimethyl-formamide / 18 h / 20 °C 6: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 7: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 0 °C 8: palladium 10% on activated carbon; formic acid; triethylamine / tetrahydrofuran; methanol / 4 h / 20 °C View Scheme | |
Multi-step reaction with 8 steps 1.1: sodium hydrogencarbonate / water; 1,4-dioxane 2.1: copper(l) iodide; caesium carbonate; L-proline; sodium methansulfinate / dimethyl sulfoxide / 9 h / 95 - 100 °C 3.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap 4.1: hydrogenchloride / dichloromethane; 1,4-dioxane / 0 °C 5.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 5.2: 18 h / 20 °C 6.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 7.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 8.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 8 steps 1: sodium hydrogencarbonate / water; 1,4-dioxane 2: copper(l) iodide; caesium carbonate; L-proline; sodium methansulfinate / dimethyl sulfoxide / 9 h / 95 - 100 °C 3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap 4: hydrogenchloride / dichloromethane; 1,4-dioxane / 0 °C 5: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 6: hydrogenchloride / water; 1,4-dioxane 7: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 8: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
(3,5-dichloro-benzylidene)-(2,2-diethoxy-ethyl)-amine
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 10 steps 1.1: sulfuric acid / dichloromethane / 7 h / 120 - 125 °C 1.2: 5 h / 0 - 50 °C / pH 12 2.1: platinum(IV) oxide / methanol / 0.17 h / 20 °C / Inert atmosphere 2.2: 25 h / 20 °C / 6464.52 Torr / Inert atmosphere 2.3: 0 - 40 °C 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 4.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 5.1: hydrogenchloride / 1,4-dioxane 6.1: sodium hydrogencarbonate 7.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 8.1: hydrogenchloride / water; 1,4-dioxane 9.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 10.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 8 steps 1.1: sulfuric acid / dichloromethane / 7 h / 120 - 125 °C 1.2: 5 h / 0 - 50 °C / pH 12 2.1: platinum(IV) oxide / methanol / 0.17 h / 20 °C / Inert atmosphere 2.2: 25 h / 20 °C / 6464.52 Torr / Inert atmosphere 2.3: 0 - 40 °C 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 4.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 5.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 5.2: 18 h / 20 °C 6.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 7.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 8.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
5,7-dichloro isoquinoline
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1.1: platinum(IV) oxide / methanol / 0.17 h / 20 °C / Inert atmosphere 1.2: 25 h / 20 °C / 6464.52 Torr / Inert atmosphere 1.3: 0 - 40 °C 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 3.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 4.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 4.2: 18 h / 20 °C 5.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 6.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 7.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 9 steps 1.1: platinum(IV) oxide / methanol / 0.17 h / 20 °C / Inert atmosphere 1.2: 25 h / 20 °C / 6464.52 Torr / Inert atmosphere 1.3: 0 - 40 °C 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 3.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 4.1: hydrogenchloride / 1,4-dioxane 5.1: sodium hydrogencarbonate 6.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 7.1: hydrogenchloride / water; 1,4-dioxane 8.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 9.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
6-hydroxy-1,2,3,4-tetrahydroisoquinoline
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 9 steps 1: N-chloro-succinimide / acetonitrile / 20 °C 2: sodium carbonate / methanol / 20 °C 3: pyridine / dichloromethane / 0.17 h / 0 - 2 °C 4: N-ethyl-N,N-diisopropylamine; 1,3-bis-(diphenylphosphino)propane; palladium diacetate / N,N-dimethyl-formamide / 20 °C / Reflux 5: sodium hydroxide / methanol / Reflux 6: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 7: hydrogenchloride / water; 1,4-dioxane 8: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 9: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
C15H16Cl2F3NO5S
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: N-ethyl-N,N-diisopropylamine; 1,3-bis-(diphenylphosphino)propane; palladium diacetate / N,N-dimethyl-formamide / 20 °C / Reflux 2: sodium hydroxide / methanol / Reflux 3: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 4: hydrogenchloride / water; 1,4-dioxane 5: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 6: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
2-(tert-butyl) 6-methyl 5,7-dichloro-3,4-dihydroisoquinoline-2,6(1Η)-dicarboxylate
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: sodium hydroxide / methanol / Reflux 2: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 3: hydrogenchloride / water; 1,4-dioxane 4: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 5: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 3 steps 1: lithium hydroxide; water / methanol / 20 °C 2: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0 - 20 °C 3: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 5 °C View Scheme | |
Multi-step reaction with 3 steps 1: lithium hydroxide; water / methanol / 20 °C 2: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0 - 20 °C 3: N-ethyl-N,N-diisopropylamine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / tetrahydrofuran / -10 - 20 °C View Scheme |
2-(tert-butoxycarbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxylic acid
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 2: hydrogenchloride / water; 1,4-dioxane 3: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 4: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 2 steps 1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0 - 20 °C 2: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 5 °C View Scheme | |
Multi-step reaction with 2 steps 1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0 - 20 °C 2: N-ethyl-N,N-diisopropylamine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / tetrahydrofuran / -10 - 20 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: sodium carbonate / N,N-dimethyl-formamide / 2 h / 25 - 35 °C 1.2: 2 h / 25 - 35 °C 2.1: triethylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate / tetrahydrofuran / 0.5 h / 25 - 35 °C 2.2: 3 h / 25 - 35 °C 3.1: pyridine; lithium iodide hydrate / 100 - 105 °C 4.1: triethylamine; HATU / N,N-dimethyl-formamide / 0.5 h / 25 - 35 °C 4.2: 2 h / 25 - 35 °C View Scheme |
C9H9Cl2NO*C7H8O3S
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1: sodium carbonate / methanol / 20 °C 2: pyridine / dichloromethane / 0.17 h / 0 - 2 °C 3: N-ethyl-N,N-diisopropylamine; 1,3-bis-(diphenylphosphino)propane; palladium diacetate / N,N-dimethyl-formamide / 20 °C / Reflux 4: sodium hydroxide / methanol / Reflux 5: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 6: hydrogenchloride / water; 1,4-dioxane 7: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 8: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
tert-butyl 5,7-dichloro-6-hydroxy-3,4-dihydroisoquinoline-2(1H)-carboxylate
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: pyridine / dichloromethane / 0.17 h / 0 - 2 °C 2: N-ethyl-N,N-diisopropylamine; 1,3-bis-(diphenylphosphino)propane; palladium diacetate / N,N-dimethyl-formamide / 20 °C / Reflux 3: sodium hydroxide / methanol / Reflux 4: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 5: hydrogenchloride / water; 1,4-dioxane 6: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 7: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 5 steps 1: pyridine / -20 - 20 °C 2: 1,3-bis-(diphenylphosphino)propane; N-ethyl-N,N-diisopropylamine; palladium diacetate / N,N-dimethyl acetamide / 20 °C 3: lithium hydroxide; water / methanol / 20 °C 4: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0 - 20 °C 5: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 5 °C View Scheme | |
Multi-step reaction with 5 steps 1: pyridine / -20 - 20 °C 2: 1,3-bis-(diphenylphosphino)propane; N-ethyl-N,N-diisopropylamine; palladium diacetate / N,N-dimethyl acetamide / 20 °C 3: lithium hydroxide; water / methanol / 20 °C 4: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0 - 20 °C 5: N-ethyl-N,N-diisopropylamine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / tetrahydrofuran / -10 - 20 °C View Scheme |
benzyl (S)-2-(5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-[3-(methylsulfonyl)phenyl]propanoate hydrochloride
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 2: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
6-hydroxybenzofuran-3-one
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 9 steps 1: triethylamine / acetone 2: sodium tetrahydroborate / methanol / 20 °C 3: hydrogenchloride; water / tetrahydrofuran / 28 °C / Inert atmosphere; Darkness 4: dichloromethane / 72 h 5: 1,3-bis-(diphenylphosphino)propane; palladium diacetate; triethylamine / N,N-dimethyl-formamide / 6 h / 70 °C / 6000.6 Torr / Autoclave 6: lithium hydroxide; water / methanol 7: oxalyl dichloride / N,N-dimethyl-formamide / 5.5 h 8: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 9: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
5,7-dichloro-1,2,3,4-tetrahydroisoquinoline hydrochloride
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 2.1: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 3.1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 0.17 h 3.2: 18 h / 20 °C 4.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C 5.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 6.1: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme | |
Multi-step reaction with 8 steps 1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1 h / 10 - 25 °C 2: n-butyllithium; N,N,N,N,-tetramethylethylenediamine 3: hydrogenchloride / 1,4-dioxane 4: sodium hydrogencarbonate 5: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide 6: hydrogenchloride / water; 1,4-dioxane 7: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 0 - 5 °C 8: triethylamine; palladium 10% on activated carbon; formic acid / tetrahydrofuran; methanol View Scheme |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
N-cyclohexyl-cyclohexanamine
Conditions | Yield |
---|---|
In tetrahydrofuran at 20℃; for 24h; | 70% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
1-isobutyric acid chloromethyl ester
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 60℃; for 16h; Sealed tube; | 61% |
1-Chloroethyl methyl carbonate
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20 - 50℃; for 38h; | 42% |
1-chloroethyl acetate
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 60℃; for 16h; Sealed tube; | 39% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 60℃; for 16h; Sealed tube; | 37% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 60℃; Sealed tube; | 36% |
propanoic acid,1-chloroethyl ester
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 60℃; for 18h; Inert atmosphere; | 35% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 60℃; for 72h; | 34% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
1-(isopropoxycarbonyloxy)ethyl chloride
Conditions | Yield |
---|---|
With potassium carbonate In N,N-dimethyl-formamide at 55℃; for 2h; | 24% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
1-chloroethyl pivalate
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 40℃; for 72h; Inert atmosphere; | 22% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 60℃; for 16h; | 4% |
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
1-Chloroethyl ethyl carbonate
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 40℃; for 20h; Inert atmosphere; | 3% |
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