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
Cas:274901-16-5
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inquiryWe are the manufacturer of this product in China. Our price is the lowest in China. CHANGZHOU HANGYU PHARMACEUTICAL TECHNOLOGY CO., LTD., founded in 1984, engages in pharmaceutical research, development, production, process design and techni
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inquiryWe can provide high quality,cheap price,spot supply and good service. If you have any questions,pls do not hesitate to contact us. Hangzhou Hysen pharma CO.,LTD. is a professional Pharmaceutical company. We are specialized in manufacturing and R&am
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inquiryDayangChem exported this product to many countries and regions at best price. If you are looking for the material's manufacturer or supplier in China, DayangChem is your best choice. Pls contact with us freely for getting detailed product spe
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inquiryWhy 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) W
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inquiryItems Standard Result Assay (Ursolic acid) 98%min 98.22% ----------------------------------------------------------------
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inquiryHebei yanxi chemical co., LTD is a professional research, development and production 2-phenylacetamide enterprise backbone members by local well-known entrepreneurs and professional senior engineers in the party's "low carbon environ
1. Guaranteed purity; 2. Large quantity in stock; 3. Largest manufacturer; 4. Best service after shipment with email; 5. High quality & competitive price; ...... Appearance:Powder Storage:-20°C Freezer Package:1kg/foil bag; 1kg/tin ;
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inquiryName Vildagliptin Synonyms (-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile Molecular Structure
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Type:Other
inquiryThe company has a professional R & D team, mature technology, very competitive prices and stable high quality products for customers to order high quality and low price product efforts! Appearance:White or off-white Solid Storage:Sealed, dry, m
The above product is Ality Chemical's strong item with best price, good quality and fast supply. Ality Chemical has been focusing on the research and production of this field for over 14 years. At the same time, we are always committed to providi
1. Factory price and high quality must be guaranteed, base on 8 years of production and R&D experience2. Free samples will be provided,ensure specifications and quality are right for customer3. Customers will receive the most professional technical s
Cas:274901-16-5
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inquiryCangzhou 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 ap
Name: Vildagliptin CAS No.: 274901-16-5 MF: C17H25N3O2 Use: Anti-diabetic agent Appearance: White powder General introduction: Vildagliptin (previously identified as LAF237, trade name ZOMELIS) is an oral anti-hyperglycemic agent (anti-diabetic
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inquiry1. We are committed to protect the integrity of our products and services. 2. Our Research and Development professional team is consisted of PhDs and Masters in biochemistry and pharmacy. 3. Our Production facility is operated by the seasoned s
Cas:274901-16-5
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inquiryHigh quality. Factory supply. In stock. Best price.1.Quick response within 24 hours;2.Best quality in your requirement;?3.We pay more attention on delivery time, and usually ship on time;4.Under the premise of safety and effectiveness, we can produce
Shanghai Seasonsgreen Chemical is a high-tech research and development, production, sale and custom synthesis set in one high-tech chemical products enterprises. Our sales and marketing division is located in Shanghai, serving international pharmaceu
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inquiryColorcom is a global leader in industrial chemical manufacturing and is continuously innovating and transforming to exceed client expectations and industry standards. Colorcom prides itself on superior customer and technical focus, while focusing on
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inquiryName:Vildagliptin CAS NO: 274901-16-5 Grade:Medical scientific research and export Molecular formula: C18H20F6N3O5P Molecular weight:503.3326802 Product Quality 12 years of chemical raw materials Mature operation of the industry System sta
Cas:274901-16-5
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Type:Other
inquiryOur company was built in 2009 with an ISO certificate.In the past 5 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:274901-16-5
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inquiryDensity: 1.27 Melting point: 153-155 C Boiling point: 531.3 ± 50.0 ° C (Predicted) Specific rotation: -78.3 ° (c=9.73 in methanol) Flash point: 275.1 ℃ Solubility: Double in DMSO (up to 45 mg/ml), in DMF (up to 20 mg/ml), or in Ethano
Cas:274901-16-5
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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
Cas:274901-16-5
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inquiryProduct Name: Vildagliptin CAS No.:274901-16-5 MF: C17H25N3O2 Purity: 99% Appearance:White powder Vildagliptin,Vildagliptin powder Appearance:White powder Storage:Store in cool and dry place, away from sun light. Package:drum Application:
Applications Lithium hydride is used as condensation agent, reducing agent, alkylation reagent and desiccant in organic synthesis, and is also a good hydrogen storage material Advantages: Hubei XinRunde Chemical Co., Ltd is a renowned
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Type:Other
inquiryHanways chempharm is a specialized company concentrating on the R&D, production, marketing and technical service of APIs and pharmaceutical intermediates. The marketing department is located in Wuhan. We have two GMP facilities in Hubei Pr
Cas:274901-16-5
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inquiry1.No Less 8 years exporting experience. Clients can 100% received goods 2.Lower Price with higher quality 3,Free sample 4,We are sincerely responsible for the "product quality" and "After Service" Upbio is Specialized
Cas:274901-16-5
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inquiryWe are the manufacturers and suppliers of API in China, and warehouse in Germany and USA of California, which can quickly and safely deliver to your address 1.High quality and competitive price. 2.Free sample for your evaluation. 3.Promptly delivery
Cas:274901-16-5
Min.Order:10 Gram
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Type:Trading Company
inquiryVildagliptin Chemical Properties Melting point 153-155 C alpha -78.3° (c = 9.73 in methanol) Boiling point 531.3±50.0 °C(Predicted) density 1.27 Fp 275.1℃ storage temp. Keep in dark place,Inert atmosphere,Store
Our company has been in existence for 10 years since its establishment. We have our own unique team. The company integrates independent research and development, production and sales. We have established famous brands at home and abroad. At present
Cas:274901-16-5
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Type:Trading Company
inquiryvildagliptin
Conditions | Yield |
---|---|
With sodium carbonate; sodium chloride In dichloromethane at 20 - 40℃; Product distribution / selectivity; | 95% |
With sodium carbonate In water at 40℃; for 0.0333333h; Product distribution / selectivity; | 75% |
vildagliptin
Conditions | Yield |
---|---|
With palladium on activated charcoal; ammonium formate In tetrahydrofuran at 20℃; for 8h; Reagent/catalyst; Solvent; Temperature; | 91.9% |
With palladium on activated charcoal; ammonium formate In tetrahydrofuran at 20℃; for 10h; Solvent; Reagent/catalyst; Temperature; | 91.9% |
(3-hydroxyadamantan-1-ylamino)acetic acid
vildagliptin
Conditions | Yield |
---|---|
Stage #1: C12H14N2O3S With sodium hydroxide In dichloromethane at 0℃; for 1.5h; Stage #2: (3-hydroxyadamantan-1-ylamino)acetic acid With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine In dichloromethane at 0℃; Concentration; | 90.8% |
Conditions | Yield |
---|---|
Stage #1: C16H33NOSi2; (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile With N-ethyl-N,N-diisopropylamine; potassium iodide In acetonitrile at 75 - 80℃; for 3h; Stage #2: With ethanol In acetonitrile for 2h; Reagent/catalyst; | 88.3% |
3-aminoadamantan-1-ol
(S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile
vildagliptin
Conditions | Yield |
---|---|
With potassium carbonate; potassium iodide In tetrahydrofuran; butanone at 40℃; for 3h; | 82% |
With potassium carbonate; potassium iodide In tetrahydrofuran; butanone at 40℃; for 3h; Reflux; | 82% |
With potassium carbonate; potassium iodide In acetone at 50 - 55℃; for 3h; Solvent; | 82.2% |
Conditions | Yield |
---|---|
Stage #1: (S)-pyrrolidine-2-carbonitrile p-toluenesulfonate; chloroacetyl chloride With triethylamine In dichloromethane at 0 - 5℃; for 2h; Stage #2: 3-aminoadamantan-1-ol In water for 4h; Temperature; Reflux; | 76.9% |
vildagliptin
Conditions | Yield |
---|---|
Stage #1: (S)-1-[2-(3-hydroxyadamantan-1-ylamino)acetyl]pyrrolidine-2-carboxylic acid amide With trifluoroacetic acid; trifluoroacetic anhydride In 2-methyltetrahydrofuran Reflux; Stage #2: With potassium carbonate In 2-methyltetrahydrofuran; water at 5 - 10℃; Reagent/catalyst; | 75% |
With trichlorophosphate In dichloromethane at 10℃; for 4h; Reagent/catalyst; Solvent; Temperature; Time; Reflux; | 4.53 g |
3-aminoadamantan-1-ol
(S)-1-(2-chloroacetyl) pyrrolidine-2-carboxamide
vildagliptin
Conditions | Yield |
---|---|
Stage #1: (S)-1-(2-chloroacetyl) pyrrolidine-2-carboxamide With trifluoroacetic anhydride In tetrahydrofuran at 20℃; for 2h; Cooling with ice; Stage #2: 3-aminoadamantan-1-ol With potassium carbonate; potassium iodide In tetrahydrofuran at 40℃; for 8.5h; Time; Reflux; | 71% |
vildagliptin
Conditions | Yield |
---|---|
With palladium 10% on activated carbon; hydrogen In methanol at 20℃; | 61.5% |
With palladium 10% on activated carbon; hydrogen In methanol for 22h; |
(S)-1-(2-chloroacetyl) pyrrolidine-2-carboxamide
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 7.82 g / trifluoroacetic anhydride / tetrahydrofuran / 1 h / 20 °C 2: K2CO3 / tetrahydrofuran / 0 - 20 °C View Scheme | |
Multi-step reaction with 2 steps 1: triethylamine; oxalyl dichloride; dimethyl sulfoxide / dichloromethane / 0.5 h / -78 °C 2: potassium carbonate; potassium iodide / tetrahydrofuran / 5 h / 60 - 65 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: 1,3,5-trichloro-2,4,6-triazine / N,N-dimethyl-formamide / 4 h / 35 - 48 °C 2.1: potassium carbonate; potassium iodide / butanone / 40 °C 2.2: 3 h / 38 - 75 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: trichlorophosphate / -5 - 20 °C 2.1: potassium carbonate; potassium iodide / acetone / 0.25 h / 20 °C 2.2: 40 - 65 °C View Scheme |
L-prolinamide
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 89 percent / K2CO3 / tetrahydrofuran 2: 7.82 g / trifluoroacetic anhydride / tetrahydrofuran / 1 h / 20 °C 3: K2CO3 / tetrahydrofuran / 0 - 20 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: trifluoroacetic anhydride / tetrahydrofuran / 3 h / 0 - 30 °C 1.2: 1 h / 0 - 5 °C 2.1: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: potassium carbonate / tetrahydrofuran / 0.17 h / 0 °C 1.2: 5 h / 0 - 20 °C 2.1: triethylamine; oxalyl dichloride; dimethyl sulfoxide / dichloromethane / 0.5 h / -78 °C 3.1: potassium carbonate; potassium iodide / tetrahydrofuran / 5 h / 60 - 65 °C View Scheme |
3-aminoadamantan-1-ol
(S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile
A
(2S)-1-{[{2[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}[(3-hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)amino]]acetyl}pyrrolidine-2-carbonitrile
B
vildagliptin
Conditions | Yield |
---|---|
With potassium carbonate; potassium iodide In tetrahydrofuran at 66℃; for 2 - 14h; Product distribution / selectivity; Heating / reflux; | |
With potassium carbonate In Isopropyl acetate at 45℃; for 14h; Product distribution / selectivity; | |
With potassium carbonate In tetrahydrofuran for 14h; Product distribution / selectivity; Heating / reflux; |
(3-hydroxyadamantan-1-ylamino)acetic acid
(2S)-pyrrolidine-2-carbonitrile
vildagliptin
Conditions | Yield |
---|---|
With dmap; dicyclohexyl-carbodiimide In dichloromethane at 20℃; for 6h; |
L-proline
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: tetrahydrofuran / 2.5 h / 65 - 70 °C 2.1: dicyclohexyl-carbodiimide / dichloromethane / 1 h / 0 - 30 °C 2.2: 3 h / 25 - 30 °C 3.1: triethylamine; oxalyl dichloride; dimethyl sulfoxide / dichloromethane / 0.5 h / -78 °C 4.1: potassium carbonate; potassium iodide / tetrahydrofuran / 5 h / 60 - 65 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: tetrahydrofuran / 3 h / Reflux 2.1: dicyclohexyl-carbodiimide / dichloromethane / 5 h / 20 °C / Cooling with ice 2.2: 6 h / 20 °C 3.1: trifluoroacetic anhydride / tetrahydrofuran / 2 h / 20 °C / Cooling with ice 3.2: 8.5 h / 40 °C / Reflux View Scheme | |
Multi-step reaction with 4 steps 1.1: tetrahydrofuran / 2.75 h / 90 °C / Cooling with ice 2.1: 1,3,5-trichloro-2,4,6-triazine / dichloromethane / 3 h / 0 °C / Reflux 2.2: 2 h 3.1: 1,3,5-trichloro-2,4,6-triazine / N,N-dimethyl-formamide / 4 h / 35 - 48 °C 4.1: potassium carbonate; potassium iodide / butanone / 40 °C 4.2: 3 h / 38 - 75 °C View Scheme |
3-aminoadamantan-1-ol
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: potassium carbonate; potassium iodide / tetrahydrofuran / 5 h / Reflux 2: potassium hydroxide; water / 12 h / 20 °C 3: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1: tetrahydrofuran / 3 h / Reflux 2: sodium tetrahydroborate; methanol / 0.5 h 3: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme | |
Multi-step reaction with 5 steps 1: water / 48 h / 20 - 30 °C 2: triethylamine; 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide / acetonitrile / 3 h / 20 - 30 °C / Inert atmosphere 3: triethylamine / dichloromethane / 5 h / 0 - 10 °C / Inert atmosphere 4: potassium carbonate; methanol / 4 h / 40 °C 5: hydrogenchloride / water / 7 h / 70 °C View Scheme |
1-Adamantanamine
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: potassium carbonate; potassium iodide / tetrahydrofuran / 5 h / Reflux 2: potassium hydroxide; potassium permanganate / water / 1.5 h / 60 - 90 °C 3: potassium hydroxide; water / 12 h / 20 °C 4: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: sulfuric acid; nitric acid / water / 5 - 25 °C 1.2: 1 h / 0 - 40 °C 2.1: potassium carbonate; potassium iodide / dichloromethane / 0.5 h / Reflux; Inert atmosphere 2.2: 6 h / Reflux 3.1: ammonia / methanol / 10 - 75 °C 4.1: trifluoroacetic anhydride; trifluoroacetic acid / 2-methyltetrahydrofuran / Reflux 4.2: 5 - 10 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: sulfuric acid; nitric acid / water / 5 - 25 °C 1.2: 1 h / 0 - 40 °C 2.1: potassium carbonate; potassium iodide / ethyl acetate / 75 °C 3.1: sodium hydroxide; water / 65 - 70 °C 4.1: 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide; N-ethyl-N,N-diisopropylamine / ethyl acetate; acetone 5.1: trifluoroacetic anhydride; trifluoroacetic acid / 2-methyltetrahydrofuran / Reflux 5.2: 5 - 10 °C View Scheme |
amantadine hydrochloride
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: nitric acid; sulfuric acid / 2 h / 0 - 12 °C 1.2: Cooling with ice 2.1: potassium carbonate; potassium iodide / tetrahydrofuran / 5 h / Reflux 3.1: potassium hydroxide; water / 12 h / 20 °C 4.1: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: nitric acid; sulfuric acid / 2 h / 0 - 12 °C 1.2: Cooling with ice 2.1: potassium carbonate; potassium iodide / tetrahydrofuran / 5 h / 60 - 65 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: nitric acid; sulfuric acid / 2 h / 0 - 12 °C 1.2: Cooling with ice 2.1: tetrahydrofuran / 3 h / Reflux 3.1: sodium tetrahydroborate; methanol / 0.5 h 4.1: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme | |
Multi-step reaction with 2 steps 1: water; sulfuric acid; nitric acid / 14 h / 0 - 20 °C 2: potassium carbonate; tetra-(n-butyl)ammonium iodide / acetonitrile / 60 °C View Scheme |
(S)-1-(2-chloroacetyl)pyrrolidine-2-carboxylic acid
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: dicyclohexyl-carbodiimide / dichloromethane / 1 h / 0 - 30 °C 1.2: 3 h / 25 - 30 °C 2.1: triethylamine; oxalyl dichloride; dimethyl sulfoxide / dichloromethane / 0.5 h / -78 °C 3.1: potassium carbonate; potassium iodide / tetrahydrofuran / 5 h / 60 - 65 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: dicyclohexyl-carbodiimide / dichloromethane / 5 h / 20 °C / Cooling with ice 1.2: 6 h / 20 °C 2.1: trifluoroacetic anhydride / tetrahydrofuran / 2 h / 20 °C / Cooling with ice 2.2: 8.5 h / 40 °C / Reflux View Scheme | |
Multi-step reaction with 3 steps 1.1: 1,3,5-trichloro-2,4,6-triazine / dichloromethane / 3 h / 0 °C / Reflux 1.2: 2 h 2.1: 1,3,5-trichloro-2,4,6-triazine / N,N-dimethyl-formamide / 4 h / 35 - 48 °C 3.1: potassium carbonate; potassium iodide / butanone / 40 °C 3.2: 3 h / 38 - 75 °C View Scheme | |
Multi-step reaction with 3 steps 1: ammonium bicarbonate; pyridine; di-tert-butyl dicarbonate / acetonitrile / 1.5 h / 25 °C 2: 1,3,5-trichloro-2,4,6-triazine / N,N-dimethyl-formamide / 4 h / 40 °C 3: potassium carbonate; potassium iodide / tetrahydrofuran; butanone / 3 h / 40 °C View Scheme |
[(3-hydroxyadamantan-1-yl)imino]acetic acid
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: sodium tetrahydroborate; methanol / 0.5 h 2: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme |
t-butyl 2-(adamantan-1-ylamino)acetate
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: potassium hydroxide; potassium permanganate / water / 1.5 h / 60 - 90 °C 2: potassium hydroxide; water / 12 h / 20 °C 3: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme |
t-butyl 2-(3-hydroxyadamantan-1-ylamino)acetate
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: potassium hydroxide; water / 12 h / 20 °C 2: dmap; dicyclohexyl-carbodiimide / dichloromethane / 6 h / 20 °C View Scheme |
1-[N-formyl-N-(3-hydroxy-1-adamantyl)aminoacetyl]pyrrolidine-2-nitrile
vildagliptin
Conditions | Yield |
---|---|
Stage #1: 1-[N-formyl-N-(3-hydroxy-1-adamantyl)aminoacetyl]pyrrolidine-2-nitrile With hydrogenchloride In water at 70℃; for 7h; Stage #2: With sodium carbonate In water Product distribution / selectivity; |
N-formyl-N-(3-hydroxy-1-adamantyl)aminoacetic acid
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: triethylamine; 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide / acetonitrile / 3 h / 20 - 30 °C / Inert atmosphere 2: triethylamine / dichloromethane / 5 h / 0 - 10 °C / Inert atmosphere 3: potassium carbonate; methanol / 4 h / 40 °C 4: hydrogenchloride / water / 7 h / 70 °C View Scheme |
1-[N-formyl-N-(3-hydroxy-1-adamantyl)aminoacetyl]pyrrolidine-2-amide
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: triethylamine / dichloromethane / 5 h / 0 - 10 °C / Inert atmosphere 2: potassium carbonate; methanol / 4 h / 40 °C 3: hydrogenchloride / water / 7 h / 70 °C View Scheme |
t-butyl 2-(3-hydroxyadamantan-1-ylamino)acetate
(S)-tert-butyl 2-carbamoylpyrrolidine-1-carboxylate
vildagliptin
Conditions | Yield |
---|---|
Stage #1: (S)-tert-butyl 2-carbamoylpyrrolidine-1-carboxylate With trifluoroacetic anhydride Stage #2: t-butyl 2-(3-hydroxyadamantan-1-ylamino)acetate |
methyl (2S)-pyrrolidine carboxylate
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: ammonium hydroxide 2.1: tetrahydrofuran 3.1: 1,3,5-trichloro-2,4,6-triazine / N,N-dimethyl-formamide / 4 h / 35 - 48 °C 4.1: potassium carbonate; potassium iodide / butanone / 40 °C 4.2: 3 h / 38 - 75 °C View Scheme |
(S)-tert-butyl 2-carbamoylpyrrolidine-1-carboxylate
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 1,3,5-trichloro-2,4,6-triazine; N,N-dimethyl-formamide / dichloromethane / 20 - 40 °C / Inert atmosphere 2: methanesulfonic acid / 40 - 45 °C 3: triethylamine / 20 - 30 °C / Inert atmosphere 4: potassium carbonate / N,N-dimethyl-formamide / 10 h / 40 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 3 steps 1.1: trifluoroacetic anhydride; triethylamine / dichloromethane / 3 h / -15 °C 2.1: acetonitrile / 10 h / 10 °C 3.1: sodium hydroxide / dichloromethane / 1.5 h / 0 °C 3.2: 0 °C View Scheme |
tert-butyl (2S)-2-cyanopyrrolidine-1-carboxylate
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: methanesulfonic acid / 40 - 45 °C 2: triethylamine / 20 - 30 °C / Inert atmosphere 3: potassium carbonate / N,N-dimethyl-formamide / 10 h / 40 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 2 steps 1.1: acetonitrile / 10 h / 10 °C 2.1: sodium hydroxide / dichloromethane / 1.5 h / 0 °C 2.2: 0 °C View Scheme | |
Multi-step reaction with 3 steps 1: methanesulfonic acid / dichloromethane / 2 h / Reflux 2: triethylamine / dichloromethane / 2 h / Reflux 3: potassium carbonate / dichloromethane / 5 h / Reflux View Scheme |
3-aminoadamantan-1-ol
vildagliptin
Conditions | Yield |
---|---|
Stage #1: 3-aminoadamantan-1-ol With potassium carbonate; potassium iodide In acetone at 20℃; for 0.25h; Stage #2: (2S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile In acetone at 40 - 65℃; Solvent; Temperature; |
vildagliptin
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: sodium hydroxide; water / methanol / 2 h / 65 °C 2: triethylamine; 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide / N,N-dimethyl-formamide; ethyl acetate / 2 h / 25 °C / Inert atmosphere 3: trifluoroacetic anhydride / 2-methyltetrahydrofuran / Inert atmosphere 4: palladium 10% on activated carbon; hydrogen / methanol / 22 h View Scheme |
(2E)-but-2-enedioic acid
vildagliptin
vildagliptin hydrogen fumarate
Conditions | Yield |
---|---|
In ethanol at 3 - 50℃; for 5h; | 97.1% |
vildagliptin
Conditions | Yield |
---|---|
In ethanol at 20 - 50℃; | 97% |
In ethanol at 20℃; for 2h; | 97% |
vildagliptin
Conditions | Yield |
---|---|
In ethanol; water; isopropyl alcohol at 35 - 40℃; Product distribution / selectivity; | 97% |
vildagliptin
Conditions | Yield |
---|---|
With calcium(II) chloride dihydrate In ethanol; water at 35 - 40℃; for 1.5h; Product distribution / selectivity; | 97% |
vildagliptin
Vildagliptin hydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride In water; isopropyl alcohol at 30 - 70℃; for 0.0833333h; | 93.8% |
zinc diacetate
vildagliptin
Conditions | Yield |
---|---|
In ethanol at 20 - 50℃; | 92% |
zinc(II) acetate dihydrate
vildagliptin
Conditions | Yield |
---|---|
In ethanol at 20℃; for 2h; | 92% |
zinc(II) chloride
vildagliptin
Conditions | Yield |
---|---|
In ethanol at 20 - 50℃; | 90% |
Conditions | Yield |
---|---|
In ethanol at 20℃; for 2h; | 90% |
vildagliptin
Conditions | Yield |
---|---|
With potassium hydroxide In water; N,N-dimethyl-formamide at 70℃; for 5h; Solvent; Reagent/catalyst; Temperature; | 90% |
With triethylamine In ethyl acetate at 90℃; for 168h; Temperature; Reagent/catalyst; Solvent; | 21% |
In 5,5-dimethyl-1,3-cyclohexadiene at 135 - 140℃; Concentration; Temperature; Solvent; | 10% |
Conditions | Yield |
---|---|
In ethanol at 3 - 45℃; for 5h; | 88% |
(S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile
vildagliptin
(2S)-1-{[{2[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}[(3-hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)amino]]acetyl}pyrrolidine-2-carbonitrile
Conditions | Yield |
---|---|
With potassium carbonate; potassium iodide In tetrahydrofuran at 20℃; for 24h; Time; Reflux; | 87% |
vildagliptin
Conditions | Yield |
---|---|
In ethanol at 20 - 50℃; | 85% |
In ethanol at 20℃; for 2h; | 85% |
zinc(II) chloride
vildagliptin
Conditions | Yield |
---|---|
In ethanol at 20 - 50℃; | 82% |
In ethanol at 20℃; for 2h; | 82% |
vildagliptin
vildagliptin hydrogen sulfate form II
Conditions | Yield |
---|---|
With sulfuric acid In butan-1-ol at 0 - 60℃; for 22.08h; | 81.3% |
With sulfuric acid In methanol at 20 - 40℃; |
vildagliptin
Conditions | Yield |
---|---|
In isopropyl alcohol at 20 - 50℃; | 78% |
vildagliptin
Conditions | Yield |
---|---|
With magnesium(II) chloride hexahydrate In isopropyl alcohol at 20℃; for 2h; | 78% |
vildagliptin
Conditions | Yield |
---|---|
In ethanol at 20 - 50℃; | 77% |
vildagliptin
Conditions | Yield |
---|---|
With strontium nitrate In ethanol at 20℃; for 2h; | 77% |
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