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inquiryLarotrectinib CAS No.:1223403-58-4 Name: Larotrectinib Synonyms: (3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide; ARRY 470; LOXO 101
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inquiryProducts Name Larotrectinib LOXO 101 CAS No. 1223403-58-4 Molecular Formula: C21H22F2N6O2 Synonyms ARRY-470; Larotrectinib Molecular Weight : 428.4351864 Packaging Specification: 25kg/drum Hubei DiBo Chemical Co., Ltd. was foun
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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 manufacturin
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inquiryWITH 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
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inquiryOur 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
Hangzhou Huarong Pharm Co., Ltd. established since 2009 , has been always focusing on supplying products and services to our clients in the field of small molecule drug. Huarong Pharm has built platforms for the research, development and manufac
Advantage : LIDE PHARMACEUTICALS LTD. is a mid-small manufacturing-type enterprise, engaged in pharmaceutical intermediates of R&D, custom-made and production, and also involving trading chemicals for export. We have established the
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inquiryLOXO-101 Chemical Properties density 1.55±0.1 g/cm3(Predicted) storage temp. RT solubility Soluble in DMSO (up to 5 mg/ml). form solid pka 8.41±0.40(Predicted) color Yellow Stability: Stable for 1 year from dat
LOXO-101 CAS:1223403-58-4 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 intermediates,
Cas:1223403-58-4
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inquiry1.High Quality: Quality is life. Quality is the most important element for all goods. We have a lab doing research in Wuhan China and produce sarms in bulk quantity. We have 8 years experience making all kinds of sarms. And all our old customers
Cas:1223403-58-4
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inquiryHenan 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 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-
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inquiryHangzhou KeyingChem Co., Ltd. exported this product to many countries and regions at best price. If you are looking for the material’s manufacturer or supplier in China, KeyingChem is your best choice. Pls contact with us freely for getting det
Zibo 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
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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
Established in May 2015, TaiChem Ltd. is initially invested by a British research and development company and started by PhDs back from aboard. The company is registered in China Medical City (CMC), Taizhou, Jiangsu Province, and the production site
Product 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,
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inquiryProduct name: LOXO-101(CAS:1223403-58-4) CAS No.:1223403-58-4 Molecule Formula:C21H22F2N6O2 Molecule Weight:428.44 Purity: 98.0% Package: 25kg/drum Description:Yellow powder Manufacture Standards:Enterprise Standard
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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
Shandong Mopai Biotechnology 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 chemicals. W
1.Applied in food field.it can improve the immune system and prolong life. 2.Appliedin cosmetic field.it can improve the skin care. 3.Applied in pharmaceutical field.it can treat various dieases. 4.Our product quality assurance will make our customer
LOXO-101 is one of the most competitive products in our company. We can supply it with good quality and best price. Appearance:powder Storage:RT Package:According to the demand of customer Application:API Port:shanghai
SAGECHEM is a chemical R&D, manufacturing and distribution company in China since 2009, including pharmaceutical intermediates, agrochemical, dyestuff intermediates, organosilicone, API and etc. We also offer a full range of services in
Advantage 1: The product passed the professional production process and quality inspection, the purity is 99% +. 2: Highly qualified engineers to provide technical documents and service. 3: We could provide sample for your test. 4: High qualit
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inquiryStock products, own laboratory Package:Grams, Kilograms Application:For R&D Transportation:According to customer request Port:Shanghai
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inquiryWe are a Union of chemistry in China, consists of chemists,engineers, laboratories,factories in China. We organize surplus capacity of R&D and production as well as custom synthesis for chemical products and chemical business project. We are supp
Cangzhou Enke Pharma Tech Co.,ltd. is located in Cangzhou City, Hebei province ,where is a famous petroleum chemical industry city in China. Enke Pharma a high-tech enterprise ,and we are dedicated to developing and manufacturing new api
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inquirywith high qualityAppearance:white powder Storage:Store in cool place. Keep container tightly closed in a dry and well-ventilated place. Package:25kg/drum Application:to formulate preparations Transportation:by courier, air or sea Port:At any port fro
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inquiry(R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine-3-amine
3-hydroxypyrrolidine
1,1'-carbonyldiimidazole
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Stage #1: 5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-amine; 1,1'-carbonyldiimidazole In dichloromethane at 20℃; for 2h; Stage #2: 3-hydroxypyrrolidine In dichloromethane for 0.0833333h; | 91% |
3-hydroxypyrrolidine
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
With triethylamine In tetrahydrofuran at 75℃; for 6h; | 91% |
(R)-(+)-2-(2,5-difluorophenyl)pyrrolidine
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In ethanol at 30℃; | 85% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: ammonium chloride; iron / ethanol; water / Inert atmosphere; Reflux 2: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 10 °C 3: ethanol / 25 °C 4: N-ethyl-N,N-diisopropylamine / ethanol / 30 °C View Scheme | |
Multi-step reaction with 4 steps 1: triethylamine / tetrahydrofuran / 5 h / 50 °C 2: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 3: triethylamine / tetrahydrofuran / 1 h / 0 °C 4: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 10 °C 2: ethanol / 25 °C 3: N-ethyl-N,N-diisopropylamine / ethanol / 30 °C View Scheme |
(R)-(+)-2-(2,5-difluorophenyl)pyrrolidine
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: triethylamine / tetrahydrofuran / 5 h / 50 °C 2: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 3: triethylamine / tetrahydrofuran / 1 h / 0 °C 4: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: triethylamine; p-toluenesulfonyl chloride / tetrahydrofuran / 12 h / 35 °C 1.2: 1 h 2.1: triethylamine / tetrahydrofuran / 5 h / 50 °C 3.1: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 4.1: triethylamine / tetrahydrofuran / 1 h / 0 °C 5.1: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
4H,5H-pyrazolo[1,5-a]pyrimidine-5-one
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: phosphorus trichloride / 6 h / 80 °C 2: nitric acid; sulfuric acid / 2 h / 0 - 5 °C 3: triethylamine / tetrahydrofuran / 5 h / 50 °C 4: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 5: triethylamine / tetrahydrofuran / 1 h / 0 °C 6: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
5-chloropyrazolo[1,5-a]pyrimidine
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: nitric acid; sulfuric acid / 2 h / 0 - 5 °C 2: triethylamine / tetrahydrofuran / 5 h / 50 °C 3: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 4: triethylamine / tetrahydrofuran / 1 h / 0 °C 5: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
(R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-nitropyrazolo[1,5-a]pyrimidine
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 2: triethylamine / tetrahydrofuran / 1 h / 0 °C 3: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
(R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine-3-amine
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: triethylamine / tetrahydrofuran / 1 h / 0 °C 2: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
(2,5-difluorophenyl)magnesium bromide
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1.1: tetrahydrofuran / 8 h / 0 - 10 °C 2.1: C25H30ClN2O2RuS; sodium formate / water; isopropyl alcohol / 12 h / 20 °C / Inert atmosphere 3.1: triethylamine; p-toluenesulfonyl chloride / tetrahydrofuran / 12 h / 35 °C 3.2: 1 h 4.1: triethylamine / tetrahydrofuran / 5 h / 50 °C 5.1: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 6.1: triethylamine / tetrahydrofuran / 1 h / 0 °C 7.1: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme | |
Multi-step reaction with 8 steps 1: tetrahydrofuran / 8 h / 0 - 10 °C 2: hydrogenchloride / tetrahydrofuran; water / 2 h / 50 °C 3: sodium formate; C25H30N2O2RuS(1+)*C32H12BF24(1-) / water; isopropyl alcohol / 12 h / 20 °C 4: hydrogenchloride / tetrahydrofuran; water / 2 h 5: triethylamine / tetrahydrofuran / 5 h / 50 °C 6: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 7: triethylamine / tetrahydrofuran / 1 h / 0 °C 8: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: C25H30ClN2O2RuS; sodium formate / water; isopropyl alcohol / 12 h / 20 °C / Inert atmosphere 2.1: triethylamine; p-toluenesulfonyl chloride / tetrahydrofuran / 12 h / 35 °C 2.2: 1 h 3.1: triethylamine / tetrahydrofuran / 5 h / 50 °C 4.1: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 5.1: triethylamine / tetrahydrofuran / 1 h / 0 °C 6.1: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme | |
Multi-step reaction with 7 steps 1: hydrogenchloride / tetrahydrofuran; water / 2 h / 50 °C 2: sodium formate; C25H30N2O2RuS(1+)*C32H12BF24(1-) / water; isopropyl alcohol / 12 h / 20 °C 3: hydrogenchloride / tetrahydrofuran; water / 2 h 4: triethylamine / tetrahydrofuran / 5 h / 50 °C 5: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 6: triethylamine / tetrahydrofuran / 1 h / 0 °C 7: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
2-(2,5-difluorophenyl)-3,4-dihydro-2H-pyrrole
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: sodium formate; C25H30N2O2RuS(1+)*C32H12BF24(1-) / water; isopropyl alcohol / 12 h / 20 °C 2: hydrogenchloride / tetrahydrofuran; water / 2 h 3: triethylamine / tetrahydrofuran / 5 h / 50 °C 4: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 5: triethylamine / tetrahydrofuran / 1 h / 0 °C 6: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
(R)-tert-butyl 2-(2,5-difluorophenyl)pyrrolidine-1-carboxylate
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: hydrogenchloride / tetrahydrofuran; water / 2 h 2: triethylamine / tetrahydrofuran / 5 h / 50 °C 3: acetic acid; hydrogen; palladium 10% on activated carbon / tetrahydrofuran / 2.5 h / 20 °C / 7600.51 Torr 4: triethylamine / tetrahydrofuran / 1 h / 0 °C 5: triethylamine / tetrahydrofuran / 6 h / 75 °C View Scheme |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
(S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
Conditions | Yield |
---|---|
With sulfuric acid In methanol at 20℃; for 0.5h; Solvent; Concentration; Temperature; Inert atmosphere; | 98.43% |
With sulfuric acid In methanol at 20℃; for 0.5h; | 94% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
With sulfuric acid In methanol at 20℃; for 0.5h; Solvent; Temperature; Time; | 98.43% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
p-toluenesulfonyl chloride
Conditions | Yield |
---|---|
With dmap; triethylamine In dichloromethane at 0 - 20℃; for 48h; Inert atmosphere; | 94.6% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
methyl trifluoromethanesulfonate
Conditions | Yield |
---|---|
Stage #1: (3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide With potassium tert-butylate In tetrahydrofuran for 0.0666667h; Inert atmosphere; Stage #2: methyl trifluoromethanesulfonate In tetrahydrofuran at 60℃; for 2h; Inert atmosphere; | 92.3% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Stage #1: (3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide With potassium tert-butylate In tetrahydrofuran for 0.0666667h; Inert atmosphere; Stage #2: [1H]-methyl trifluoromethanesulfonate In tetrahydrofuran at 60℃; Inert atmosphere; | 92.3% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
With hydrogenchloride In ethanol; tert-butyl methyl ether; water at 50℃; | 89% |
With hydrogenchloride In ethanol; tert-butyl methyl ether at 50℃; for 4h; Inert atmosphere; | 89% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
With hydrogen bromide In ethanol; tert-butyl methyl ether; water at 50℃; Reflux; | 85% |
With hydrogen bromide In ethanol; tert-butyl methyl ether; water at 50℃; Inert atmosphere; | 85% |
2,2-difluoro-2-(fluorosulfonyl)acetic acid
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
With copper(l) iodide In acetonitrile at 50℃; for 1.25h; Inert atmosphere; | 82.3% |
methanesulfonic acid
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
In ethanol; tert-butyl methyl ether at 50℃; Reflux; | 78% |
In ethyl acetate at 20 - 50℃; for 48h; |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
With methanesulfonic acid In ethanol; tert-butyl methyl ether at 50℃; Inert atmosphere; | 78% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
2-fluoroethyl tosylate
Conditions | Yield |
---|---|
Stage #1: (3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide With potassium carbonate In ethanol at 20℃; for 0.25h; Stage #2: 2-fluoroethyl tosylate In ethanol at 70℃; for 18h; | 46% |
fluoromethyl-d2 4-methylbenzenesulfonate
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
Stage #1: (3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide With potassium tert-butylate In acetonitrile at 20℃; for 0.25h; Inert atmosphere; Stage #2: fluoromethyl-d2 4-methylbenzenesulfonate In acetonitrile at 20℃; for 2.91667h; Inert atmosphere; Stage #3: With tetrabutyl ammonium fluoride In acetonitrile at 20℃; for 18h; Inert atmosphere; | 29.2% |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
With hydrogenchloride In ethanol; water at 5 - 15℃; for 5h; Temperature; |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
Conditions | Yield |
---|---|
In ethanol; tert-butyl methyl ether Reflux; |
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide
(1S)-10-camphorsulfonic acid
Conditions | Yield |
---|---|
In ethanol; tert-butyl methyl ether Reflux; Inert atmosphere; |
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