zhenyu biotech exported this product to many countries and regions at best price. if you are looking for the material's manufacturer or supplier in china, zhenyu biotech is your best choice. pls contact with us freely for getting detailed produc
Cas:486460-32-6
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inquiryHigh quality products. Always supply highest grade to you. Purity:≥99% Reasonable & Competitive Price. Huge capacity determines the lowest shared cost. The more you buy the more competitive prices you will get. The sincerest and most pro
Cas:486460-32-6
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inquirySitagliptin CAS No.:486460-32-6 Name: Sitagliptin Synonyms: (3R)-3-Amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one Molecular Structure Molecular Formula: C
Cas:486460-32-6
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inquiryHangzhou 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
Cas:486460-32-6
Min.Order:1 Gram
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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) We c
Cas:486460-32-6
Min.Order:1 Kilogram
FOB Price: $25.0 / 800.0
Type:Trading Company
inquiryWelcome to Simagchem, your partner in China as a premier supply of bulk specialty chemicals for industry and life science. We introduce experienced quality product and exceptional JIT service with instant market intelligence in China to benefit our
Cas:486460-32-6
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inquiryWe can provide GMP validation service that complies with SFDA, FDA, WHO and EU EMPA.Excellent registration team could help us easlily to register our products in different countries.If you and your customer are interested in some products or need C
Cas:486460-32-6
Min.Order:1 Gram
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Type:Manufacturers
inquiryUnique advantages for Sitagliptin Cas 486460-32-6 Guaranteed purity High quality & competitive price Quality control Fast feedback Prompt shipment Appearance:Off-white to white powder Storage:Cool dry place Package:1kg/foill bag
Cas:486460-32-6
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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
Cas:486460-32-6
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inquiry1. 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:486460-32-6
Min.Order:1 Gram
FOB Price: $0.1
Type:Manufacturers
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 api, intermedi
1. Pharm grade grade 2. IN STOCK 3. FAST REPLY QUALIFED ; EFFICIENCY; RESPONSIBLE Package:25kg/drum Application:active pharmaceutical ingredient Transportation:as request
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
Cas:486460-32-6
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Type:Manufacturers
inquiryDayangchem's 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. DayangChem can provide different quantities
Cas:486460-32-6
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inquiry
Cas:486460-32-6
Min.Order:1 Metric Ton
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Type:Manufacturers
inquiryProduct Name: Sitagliptin Synonyms: Sitagliptin free base;(3R)-3-AMino-1-[3-(trifluoroMethyl)-5,6,7,8-tetrahydro-1,2,4-riazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-rifluorophenyl) butan-1-one;(R)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[
Cas:486460-32-6
Min.Order:1 Kilogram
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Type:Lab/Research institutions
inquiryAdvantage : 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 R&
Cas:486460-32-6
Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryOur advantages: 1. All inquiries will be replied within 12 hours. 2. Dedication to quality, supply & service. 3. Strictly on selecting raw materials. 4. Reasonable & competitive price, fast lead time. 5. Sample is available for your eva
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Cas:486460-32-6
Min.Order:1 Kilogram
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Type:Trading Company
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
Product Name: Sitagliptin Manufacture Date: 05th,Feb.,2023 Analysis Date: 05th,Feb.,2023 Expiry Date: 04th,Feb.,2025 Storage: Store in cool&dry place, in well-closed containers. Appearance:White powder Storage:Store in cool and dry place, away
Appearance:white to light yellow powder Storage:room temperature Package: 25kg/drum Application:Sitagliptin is a useful pharmaceutical drug. Could be useful for treating intestinal inflammation, diabetes, pre- diabetes, impaired glucose tolerance, h
Cas:486460-32-6
Min.Order:1 Kilogram
Negotiable
Type:Lab/Research institutions
inquiryAdvantages: Hubei XinRunde Chemical Co., Ltd is a renowned pharmaceutical manufacturer. We can offer high quality products at competitive price in quick delivery with 100% custom pass guaranteed. Never stop striving to offer our best serv
Cas:486460-32-6
Min.Order:10 Gram
Negotiable
Type:Other
inquiryWe are concentrating on APIs and pharmaceutical intermediates. With in depth knowledge and understanding in this industry, we are indulged in supplying a wide assortments of Sitagliptin from Wuhan, Hubei, China. It is made obt
1,In No Less five years exporting experience. 2.Lower Price with higher quality 3,Free sample 4,We are sincerely responsible for the "product quality" and "After Service" Onchem specialized in APIs, chemical intermediate
Cas:486460-32-6
Min.Order:25 Kilogram
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Type:Lab/Research institutions
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:486460-32-6
Min.Order:10 Gram
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Type:Trading Company
inquiryMethanesulfonic acid is a raw material for medicine and pesticide. It can also be used as dehydrating agent, curing accelerator for coating, treating agent for fiber, solvent, catalysis, and esterification as well as polymerization reaction. It c
Cas:486460-32-6
Min.Order:1 Kilogram
FOB Price: $86.0 / 89.0
Type:Trading Company
inquirySitagliptin CAS: 486460-32-6 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 intermediat
Cas:486460-32-6
Min.Order:1 Gram
Negotiable
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
(R)-benzyl (4-oxo-4-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-yl)carbamate
sitagliptin
Conditions | Yield |
---|---|
With hydrogen; palladium 10% on activated carbon In tetrahydrofuran at 20℃; under 760.051 Torr; | 100% |
With hydrogen; palladium-on-charcoal In tetrahydrofuran; water at 20℃; under 760.051 Torr; | 100% |
With hydrogen; palladium 10% on activated carbon In methanol | 99% |
With methylmagnesium bromide; hydrogen; palladium diacetate; nickel diacetate In water at 45℃; for 20h; | 79% |
7-(1-oxo-3((R)-amino)-4-(2,4,5-trifluorophenyl)butyl)-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazine di-p-tolyl-L-tartarate
sitagliptin
Conditions | Yield |
---|---|
With sodium hydroxide In ethyl acetate at 10℃; Product distribution / selectivity; | 99.5% |
sitagliptin
Conditions | Yield |
---|---|
With formic acid; Pt/Al2O3; hydrogen In methanol at 20℃; Autoclave; Large scale; | 97.8% |
Stage #1: (3R)-3-[(benzyIoxy)amino]-l-[3-(trifluoromethyl)-5H,6H,7H,8H [1 ,2,4] triazolo [4,3-a] pyrazin-7-yl]-4-(2,4,5-trifluorophenyl) butan-1-one With hydrogenchloride; palladium 10% on activated carbon In ethanol; water at 30℃; under 2068.65 Torr; for 12 - 14h; Stage #2: With sodium hydroxide In ethanol; water at 12 - 14℃; pH=13; Stage #3: With phosphoric acid In ethanol; water at 45℃; | 66% |
(Z)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)but-2-en-1-one
sitagliptin
Conditions | Yield |
---|---|
Stage #1: (Z)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)but-2-en-1-one With ammonium chloride; chloro(1,5-cyclooctadiene)rhodium(I) dimer; (R)-1-[(S)-2-(di-tert-butylphosphino)ferrocenyl]ethyl-di-2-methylphenylphosphine In methanol at 20℃; for 1h; Stage #2: With hydrogen In methanol at 50℃; under 5171.62 Torr; for 18h; Product distribution / selectivity; | 97% |
With di-μ-chloro-bis(1,5-cyclooctadiene)dirhodium; hydrogen; (R,S)-t-bu Josiphos In methanol at 20 - 50℃; under 10343.2 Torr; for 14h; | 93% |
With chloro(1,5-cyclooctadiene)rhodium(I) dimer; (2S)-1-[(1S)-1-[bis(1,1-dimethylethyl)phosphino]ethyl]-2-(diphenylphosphino)ferrocene; hydrogen; ammonium chloride In methanol at 50℃; under 13689.1 Torr; Inert atmosphere; enantioselective reaction; | 82% |
3-trifluoromethyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine
sitagliptin
Conditions | Yield |
---|---|
With triethylamine In tetrahydrofuran for 1h; Reflux; | 97% |
(R)-tert-butyl 4-oxo-4-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-ylcarbamate
sitagliptin
Conditions | Yield |
---|---|
With hydrogenchloride In isopropyl alcohol at 20 - 25℃; | 96.88% |
With hydrogenchloride In methanol at 15 - 45℃; for 3h; | 95.81% |
With hydrogenchloride; methanol In water at 50℃; for 4h; | 95% |
C23H21F6N5O
sitagliptin
Conditions | Yield |
---|---|
With Pt/Al2O3; hydrogen; acetic acid In methanol at 20℃; Autoclave; Large scale; | 96.7% |
(3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid
3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride
sitagliptin
Conditions | Yield |
---|---|
Stage #1: (3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid With triethylamine In dichloromethane for 0.166667h; Stage #2: With benzotriazol-1-ol; dicyclohexyl-carbodiimide In dichloromethane at 25 - 30℃; for 4h; Stage #3: 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride Further stages; | 96.5% |
(R,R)-N-benzyl-N-(α-methylbenzyl)-1-(2',4',5'-trifluorophenyl)-4-oxo-4-{3''-(trifluoromethyl)-5'',6''-dihydro-1'',2'',4''-triazolo[4,3-α]pyrazin-7''(8''H)-yl}butan-2-amine
sitagliptin
Conditions | Yield |
---|---|
With 30% w/w Pd(OH)2/C; hydrogen In methanol under 3800.26 Torr; for 24h; | 96% |
With 5%-palladium/activated carbon; hydrogen; acetic acid In methanol at 50℃; under 19001.3 Torr; for 48h; | 95% |
(3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid
sitagliptin
Conditions | Yield |
---|---|
Stage #1: (3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid With thionyl chloride In ethyl acetate at 26℃; for 2h; Stage #2: 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-α]pyrazine hydrochloride With triethylamine In ethyl acetate at 25℃; Solvent; Temperature; | 96% |
Stage #1: 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-α]pyrazine hydrochloride; (3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid With 1-methyl-1H-imidazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride at 0 - 20℃; for 16h; Stage #2: With hydrogenchloride In ethanol at 20℃; for 18h; Stage #3: With sodium hydroxide In ethanol; water pH=10 - 12; Time; Solvent; | 90% |
Stage #1: (3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid With pivaloyl chloride; sodium carbonate In toluene Cooling; Stage #2: 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-α]pyrazine hydrochloride In toluene Stage #3: With hydrogenchloride In water; toluene Reagent/catalyst; | 4.4 g |
sitagliptin
Conditions | Yield |
---|---|
In water at 20 - 25℃; pH=8 - 9; Alkaline conditions; | 96% |
(2S)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine dihydrogenphosphate salt
sitagliptin
Conditions | Yield |
---|---|
With sodium hydroxide In water at 0 - 5℃; for 1h; | 95% |
3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride
sitagliptin
Conditions | Yield |
---|---|
With 2-Ethylhexanoic acid; triethylamine In tetrahydrofuran at 75℃; for 72h; | 95% |
With 2-Ethylhexanoic acid; triethylamine In tetrahydrofuran at 75℃; for 72h; Solvent; Temperature; Reagent/catalyst; Concentration; | 95% |
(3R)-3-[[(1R)-1-phenylethyl]amino]-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
sitagliptin
Conditions | Yield |
---|---|
With 20% palladium hydroxide-activated charcoal; hydrogen; acetic acid In methanol; water at 50℃; under 7500.75 Torr; for 14h; | 94% |
With palladium 10% on activated carbon; hydrogen; acetic acid In methanol; water at 50℃; under 7500.75 Torr; for 14h; | 81.2% |
With formic acid; palladium(II) hydroxide/carbon In tetrahydrofuran; methanol; water at 60℃; for 6h; | 79.4% |
sitagliptin
Conditions | Yield |
---|---|
In water at 20 - 25℃; pH=8 - 9; Alkaline conditions; | 93.5% |
sitagliptin
Conditions | Yield |
---|---|
In water at 20 - 25℃; pH=8 - 9; Alkaline conditions; | 93% |
sitagliptin sulfate
sitagliptin
Conditions | Yield |
---|---|
In water | 92% |
1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butane-1,3-dione
sitagliptin
Conditions | Yield |
---|---|
Stage #1: 1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butane-1,3-dione With ammonium formate; chloro(1,5-cyclooctadiene)rhodium(I) dimer; (R)-1-[(S)-2-(di-tert-butylphosphino)ferrocenyl]ethyl-di-2-methylphenylphosphine In methanol at 55℃; for 5h; Stage #2: With hydrogen In methanol at 55℃; under 12929 Torr; for 20h; Product distribution / selectivity; | 91% |
Multi-step reaction with 3 steps 1: isopropyl alcohol; acetic acid / 18 h / 50 °C 2: sodium tetrahydroborate; acetic acid / tetrahydrofuran / 3 h / 20 °C 3: 20% palladium hydroxide-activated charcoal; hydrogen; acetic acid / methanol; water / 14 h / 50 °C / 7500.75 Torr View Scheme | |
Multi-step reaction with 3 steps 1: isopropyl alcohol; acetic acid / 18 h / 50 °C 2: sodium tetrahydroborate; formic acid / tetrahydrofuran / -30 °C 3: 20% palladium hydroxide-activated charcoal; hydrogen; acetic acid / methanol; water / 14 h / 50 °C / 7500.75 Torr View Scheme |
(R)-N-benzyl-1-(2',4',5'-trifluorophenyl)-4-oxo-4-{3''-(trifluoromethyl)-5'',6''-dihydro-1'',2'',4''-triazolo[4,3-α]pyrazin-7''(8''H)-yl}butan-2-amine
sitagliptin
Conditions | Yield |
---|---|
With 20 wt.% Pd(OH)2 on activated carbon; hydrogen In methanol under 3800.26 Torr; for 24h; | 91% |
(R)-2-methyl-N-((R)-4-oxo-4-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4] triazolo[4,3-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-yl)propane-2-sulfinamide
sitagliptin
Conditions | Yield |
---|---|
With hydrogenchloride; methanol In water at 48℃; | 91% |
With hydrogenchloride In 1,4-dioxane at 20℃; for 4h; Solvent; | 90.7% |
With hydrogenchloride; water In methanol at 20℃; for 4h; | 89% |
With hydrogenchloride In water at 70℃; for 2h; | 89% |
With hydrogenchloride In methanol; water at 20℃; for 4h; |
sitagliptin
Conditions | Yield |
---|---|
Stage #1: C17H13F6N5O2 With water In ethanol at 80℃; for 2h; Stage #2: With copper In quinoline; ethanol at 140℃; for 3h; | 91% |
(R)-3-azido-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
sitagliptin
Conditions | Yield |
---|---|
Stage #1: (R)-3-azido-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one With triphenylphosphine In tetrahydrofuran at 50℃; for 2h; Stage #2: With ammonium hydroxide In tetrahydrofuran; water for 10h; | 90% |
Stage #1: (R)-3-azido-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one With triphenylphosphine In tetrahydrofuran at 50℃; for 2h; Stage #2: With ammonium hydroxide In tetrahydrofuran; water for 10h; | 86% |
With hydrogen; palladium on carbon In methanol for 6h; |
sitagliptin
Conditions | Yield |
---|---|
In water at 20 - 25℃; pH=8 - 9; Alkaline conditions; | 90% |
sitagliptin
Conditions | Yield |
---|---|
With palladium 10% on activated carbon; hydrogen In water; isopropyl alcohol at 65 - 70℃; under 5430.2 Torr; for 8 - 10h; Inert atmosphere; | 88% |
sitagliptin
Conditions | Yield |
---|---|
With ammonia In water at 25℃; pH=10; Product distribution / selectivity; | 87.3% |
With potassium hydroxide In tert-butyl methyl ether; water at 0 - 20℃; pH=11; | 85% |
With sodium hydroxide In water at 0 - 5℃; for 1h; | |
With sodium hydrogencarbonate; sodium chloride In water; ethyl acetate at 25 - 42℃; Reagent/catalyst; Temperature; | 1.8 g |
(R)-3-nitro-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
sitagliptin
Conditions | Yield |
---|---|
Stage #1: (R)-3-nitro-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one With hydrogenchloride; zinc In methanol; water at 20℃; for 0.5h; Stage #2: With sodium hydroxide In methanol; water pH=10; | 87% |
3(R)-3-[(benzyloxy)amino]-1-[3-(trifluoromethyl)-5H,6H,7H,8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
sitagliptin
Conditions | Yield |
---|---|
With palladium 10% on activated carbon; hydrogen In ethanol; water at 50℃; under 2068.65 Torr; Large scale; | 86% |
Multi-step reaction with 2 steps 1: phosphoric acid / isopropyl alcohol / 16 h / 30 °C 2: sodium hydroxide / water / 1 h / 0 - 5 °C View Scheme | |
With palladium 10% on activated carbon; hydrogen In ethanol; water at 50℃; under 2280.15 Torr; for 12h; |
(R)-3-amino-4-phenyl(2,4,5-trifluorophenyl)butanoic acid
3-trifluoromethyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine
sitagliptin
Conditions | Yield |
---|---|
With 4-methyl-morpholine; benzotriazol-1-ol In ethanol; dichloromethane at 10 - 25℃; for 3h; | 86% |
(2S)-2({(1R)-3-oxo-1-(2,4,5-trifluorobenzyl)-3-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl]propyl}amino)-2-phenylethanamide
sitagliptin
Conditions | Yield |
---|---|
With 20% palladium hydroxide-activated charcoal; hydrogen; acetic acid In methanol; water at 50℃; under 7500.75 Torr; for 14h; | 85% |
(3R)-3-[[(1R)-1-phenylethyl]amino]-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
sitagliptin
Conditions | Yield |
---|---|
Stage #1: (3R)-3-[[(1R)-1-phenylethyl]amino]-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one With formic acid; 10 wt% Pd(OH)2 on carbon In tetrahydrofuran; methanol for 6h; Reflux; Stage #2: With phosphoric acid In ethanol; water; ethyl acetate at 50 - 74℃; for 1.5h; Stage #3: sitagliptin phosphate In ethanol; water at 65℃; for 1h; | 67.1% |
Conditions | Yield |
---|---|
In acetonitrile at 25 - 75℃; Product distribution / selectivity; | 99% |
In water at 35 - 37℃; for 0.166667h; |
sitagliptin
sitagliptin phosphate monohydrate
Conditions | Yield |
---|---|
With phosphoric acid In water; isopropyl alcohol at 70 - 80℃; for 2h; Temperature; | 97.7% |
With phosphoric acid; water In isopropyl alcohol at 20 - 75℃; | 95% |
With phosphoric acid; water In isopropyl alcohol at 75℃; |
Conditions | Yield |
---|---|
In ethyl acetate at 25 - 50℃; Product distribution / selectivity; | 97% |
sitagliptin
Conditions | Yield |
---|---|
With phosphoric acid In ethanol at 80℃; optical yield given as %ee; | 96% |
With phosphoric acid In ethanol at 80℃; for 0.5h; | 96% |
With phosphoric acid; water In isopropyl alcohol at 70 - 80℃; | 96% |
sitagliptin
(R)-3-azido-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
Conditions | Yield |
---|---|
With fluorosulfonyl azide; potassium hydrogencarbonate In tert-butyl methyl ether; water; N,N-dimethyl-formamide at 20℃; for 0.0833333h; | 96% |
Adipic acid
sitagliptin
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine adipic acid
Conditions | Yield |
---|---|
In isopropyl alcohol at 25 - 50℃; for 0.5h; | 95.9% |
In isopropyl alcohol at 25 - 50℃; | 95.9% |
In ethanol at 25 - 80℃; | 56.8% |
Conditions | Yield |
---|---|
In methanol at 25 - 32℃; for 1h; | 95% |
In ethyl acetate; isopropyl alcohol at 25.5 - 26.7℃; for 0.683333h; | 91% |
In isopropyl alcohol at 30℃; Reflux; | |
In acetonitrile at 25 - 50℃; Product distribution / selectivity; | |
In butanone at 20℃; for 1h; Product distribution / selectivity; |
Conditions | Yield |
---|---|
In ethanol | 95% |
sitagliptin
Conditions | Yield |
---|---|
With sulfuric acid In tert-butyl methyl ether; acetonitrile at 20℃; | 95% |
With sulfuric acid In acetonitrile at 25 - 50℃; Product distribution / selectivity; |
sitagliptin
Conditions | Yield |
---|---|
With sulfuric acid In ethanol for 0.766667h; | 94.8% |
benzenesulfonic acid
sitagliptin
Conditions | Yield |
---|---|
In methanol at 25 - 32℃; for 1h; | 93% |
In Isopropyl acetate at 50℃; for 1h; | |
In Isopropyl acetate at 45 - 50℃; | 0.63 g |
sitagliptin
Conditions | Yield |
---|---|
With phosphoric acid In water; isopropyl alcohol at 20 - 60℃; for 1.5h; | 92.6% |
With phosphoric acid In methanol | |
With phosphoric acid In water; isopropyl alcohol at 25 - 78℃; | 6.7 g |
sitagliptin
Conditions | Yield |
---|---|
With hydrogenchloride In water; isopropyl alcohol at 20℃; for 0.75h; | 92.4% |
With hydrogenchloride In isopropyl alcohol at 30℃; for 3h; | |
With isopropyl alcohol hydrogen chloride In methanol; diethyl ether at 25 - 45℃; for 1h; | 1.1 g |
With hydrogenchloride In water; ethyl acetate at 0 - 65℃; Solvent; Temperature; | 102 g |
With hydrogenchloride In isopropyl alcohol at 50℃; Temperature; Solvent; | 10.3 g |
sitagliptin
Conditions | Yield |
---|---|
In methanol; water; isopropyl alcohol at 20℃; | 92% |
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