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TAIZHOU ZHENYU BIOTECHNOLOGY CO., LTD

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

High Quality Sitagliptin 486460-32-6 Manufacturer

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Lab/Research institutions

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Hangzhou Johoo Chemical Co., Ltd

High 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

High quality Sitagliptin supplier/Sitagliptin base/Intermeidate of SitagliPtin/Sitagliptin-D4 in China

Cas:486460-32-6

Min.Order:1 Metric Ton

FOB Price: $5.5 / 6.5

Type:Trading Company

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Hangzhou Think Chemical Co. Ltd

Sitagliptin 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

High purity Sitagliptin base CAS No.:486460-32-6

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $2.0

Type:Other

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Hangzhou Huarong Pharm Co., Ltd.

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

Sitagliptin base TOP1 supplier in the world

Cas:486460-32-6

Min.Order:1 Gram

FOB Price: $1.0 / 2.0

Type:Lab/Research institutions

inquiry

Sinoway Industrial Co., Ltd.

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

High Quality 99% Sitagliptin phosphate monohydrate

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $25.0 / 800.0

Type:Trading Company

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Simagchem Corporation

Welcome 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

High quality Sitagliptin supplier in China

Cas:486460-32-6

Min.Order:0 Metric Ton

Negotiable

Type:Manufacturers

inquiry

Hangzhou JINLAN Pharm-Drugs Technology Co., Ltd

We 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

Sitagliptin manufacturer with low price

Cas:486460-32-6

Min.Order:1 Gram

Negotiable

Type:Manufacturers

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Wuhan Fortuna Chemical Co.,Ltd

Unique 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

Factory supply Sitagliptin Cas 486460-32-6 with high quality and best price

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $500.0 / 575.0

Type:Trading Company

inquiry

Henan Allgreen Chemical Co.,Ltd

The 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

Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

Negotiable

Type:Manufacturers

inquiry

Ality Chemical Corporation

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

Xi'an Xszo Chem Co., Ltd.

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

High Quality 99% Sitagliptin 486460-32-6 ISO Producer

Cas:486460-32-6

Min.Order:1 Gram

FOB Price: $0.1

Type:Manufacturers

inquiry

Enke Pharma-tech Co.,Ltd. (Cangzhou, China )

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, intermedi

Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Manufacturers

inquiry

HANGZHOU CLAKE BIOTECH CO.,LTD

1. Pharm grade grade 2. IN STOCK 3. FAST REPLY QUALIFED ; EFFICIENCY; RESPONSIBLE Package:25kg/drum Application:active pharmaceutical ingredient Transportation:as request

Sitagliptin

Cas:486460-32-6

Min.Order:25 Kilogram

Negotiable

Type:Trading Company

inquiry

Shanghai Seasonsgreen Chemical Co.,Ltd

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

lower price High quality Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Manufacturers

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Dayang Chem (Hangzhou) Co.,Ltd.

Dayangchem'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

Sitagliptin Manufacturer/High quality/Best price/In stock

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $3.0

Type:Lab/Research institutions

inquiry

Chemwill Asia Co., Ltd.

Sitagliptin -- CHemwill

Cas:486460-32-6

Min.Order:1 Metric Ton

FOB Price: $1.0

Type:Manufacturers

inquiry

Henan Tianfu Chemical Co., Ltd.

Product 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[

486460-32-6 Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $150.0

Type:Lab/Research institutions

inquiry

LIDE PHARMACEUTICALS LIMITED

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 R&amp

Sitagliptin / LIDE PHARMA- Factory supply / Best price

Cas:486460-32-6

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Hebei Nengqian Chemical Import and Export Co., LTD

Our 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

Sitagliptin

Cas:486460-32-6

Min.Order:1 Gram

FOB Price: $12.0 / 15.0

Type:Trading Company

inquiry

Zhuozhou Wenxi import and Export Co., Ltd

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

Factory direct supply CAS 486460-32-6 with best quality

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $139.0 / 210.0

Type:Trading Company

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Wuhan Han Sheng New Material Technology Co.,Ltd

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

Sitagliptin

Cas:486460-32-6

Min.Order:10 Kilogram

Negotiable

Type:Trading Company

inquiry

Henan Sinotech Import&Export Corporation

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

Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Other

inquiry

Hangzhou Sartort Biopharma Co., Ltd

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

factory price Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

inquiry

Hubei Langyou International Trading Co., Ltd

Advantages: 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

HANWAYS CHEMPHARM CO.,LIMITED

We 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

Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Trading Company

inquiry

Shanghai Upbio Tech Co.,Ltd

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

Sitagliptin CAS NO.486460-32-6

Cas:486460-32-6

Min.Order:25 Kilogram

FOB Price: $1.0

Type:Lab/Research institutions

inquiry

Xi'an Faithful Biotech Co., Ltd.

We 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

High Purity Wholesale Simvastatin Base Raw Material with 99% Purity Simvastatin

Cas:486460-32-6

Min.Order:10 Gram

FOB Price: $3.5

Type:Trading Company

inquiry

Baoji Guokang Healthchem co.,ltd

Methanesulfonic 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

Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

FOB Price: $86.0 / 89.0

Type:Trading Company

inquiry

Qingdao Beluga Import and Export Co., LTD

Sitagliptin 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

Sitagliptin CAS: 486460-32-6

Cas:486460-32-6

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Shandong Hanjiang Chemical Co., Ltd.

Hello, 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

Sitagliptin

Cas:486460-32-6

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

inquiry

Synthetic route

(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
1242069-63-1

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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 methanol99%
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
1169707-28-1

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
486460-32-6

sitagliptin

Conditions
ConditionsYield
With sodium hydroxide In ethyl acetate at 10℃; Product distribution / selectivity;99.5%
(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

(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

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
767340-03-4

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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%
C14H13F3N2O4

C14H13F3N2O4

3-trifluoromethyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine
486460-21-3

3-trifluoromethyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
486460-23-5

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
1306610-49-0

C23H21F6N5O

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
486460-00-8

(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
762240-92-6

3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
1380521-88-9

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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%
3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-α]pyrazine hydrochloride

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
486460-00-8

(3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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 hydrochloride

Sitagliptin hydrochloride

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
823817-58-9

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
With sodium hydroxide In water at 0 - 5℃; for 1h;95%
(4R)-4-(2,4,5-trifluorobenzyl)azetidin-2-one

(4R)-4-(2,4,5-trifluorobenzyl)azetidin-2-one

3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride
762240-92-6

3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
1169707-30-5

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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 phosphate

sitagliptin phosphate

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
In water at 20 - 25℃; pH=8 - 9; Alkaline conditions;93.5%
sitagliptin sulfate

sitagliptin sulfate

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
In water at 20 - 25℃; pH=8 - 9; Alkaline conditions;93%
sitagliptin sulfate
1169707-31-6

sitagliptin sulfate

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
In water92%
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
764667-65-4

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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
1393363-87-5

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
1349649-83-7

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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;
C17H13F6N5O2

C17H13F6N5O2

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
1253055-98-9

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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 succinate

sitagliptin succinate

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
In water at 20 - 25℃; pH=8 - 9; Alkaline conditions;90%
(R)-3-(((R)-1-phenylethyl)amino)-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 hydrochloride

(R)-3-(((R)-1-phenylethyl)amino)-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 hydrochloride

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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 phosphate

sitagliptin phosphate

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
1351564-29-8

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
1361389-75-4

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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
936630-57-8

(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
486460-21-3

3-trifluoromethyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine

sitagliptin
486460-32-6

sitagliptin

Conditions
ConditionsYield
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
769195-20-2

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
With 20% palladium hydroxide-activated charcoal; hydrogen; acetic acid In methanol; water at 50℃; under 7500.75 Torr; for 14h;85%
sitagliptin phosphate

sitagliptin phosphate

(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
1169707-30-5

(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
486460-32-6

sitagliptin

Conditions
ConditionsYield
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%
orotic acid
65-86-1

orotic acid

sitagliptin
486460-32-6

sitagliptin

sitagliptin orotate
1246343-77-0

sitagliptin orotate

Conditions
ConditionsYield
In acetonitrile at 25 - 75℃; Product distribution / selectivity;99%
In water at 35 - 37℃; for 0.166667h;
sitagliptin
486460-32-6

sitagliptin

sitagliptin phosphate monohydrate
654671-77-9

sitagliptin phosphate monohydrate

Conditions
ConditionsYield
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℃;
(R)-Mandelic Acid
611-71-2

(R)-Mandelic Acid

sitagliptin
486460-32-6

sitagliptin

sitagliptin (R)-(-)mandelate
1240038-86-1

sitagliptin (R)-(-)mandelate

Conditions
ConditionsYield
In ethyl acetate at 25 - 50℃; Product distribution / selectivity;97%
sitagliptin
486460-32-6

sitagliptin

sitagliptin phosphate

sitagliptin phosphate

Conditions
ConditionsYield
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
486460-32-6

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
1253055-98-9

(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
ConditionsYield
With fluorosulfonyl azide; potassium hydrogencarbonate In tert-butyl methyl ether; water; N,N-dimethyl-formamide at 20℃; for 0.0833333h;96%
Adipic acid
124-04-9

Adipic acid

sitagliptin
486460-32-6

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
1417158-34-9

(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
ConditionsYield
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%
(2E)-but-2-enedioic acid
110-17-8

(2E)-but-2-enedioic acid

sitagliptin
486460-32-6

sitagliptin

Sitagliptin fumarate
837430-24-7

Sitagliptin fumarate

Conditions
ConditionsYield
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;
(S)-Mandelic acid
17199-29-0

(S)-Mandelic acid

sitagliptin
486460-32-6

sitagliptin

sitagliptin L-mandelate

sitagliptin L-mandelate

Conditions
ConditionsYield
In ethanol95%
sitagliptin
486460-32-6

sitagliptin

sitagliptin hydrogensulfate

sitagliptin hydrogensulfate

Conditions
ConditionsYield
With sulfuric acid In tert-butyl methyl ether; acetonitrile at 20℃;95%
With sulfuric acid In acetonitrile at 25 - 50℃; Product distribution / selectivity;
sitagliptin
486460-32-6

sitagliptin

sitagliptin sulfate

sitagliptin sulfate

Conditions
ConditionsYield
With sulfuric acid In ethanol for 0.766667h;94.8%
benzenesulfonic acid
98-11-3

benzenesulfonic acid

sitagliptin
486460-32-6

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 besylate

(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 besylate

Conditions
ConditionsYield
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
486460-32-6

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 phosphate

(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 phosphate

Conditions
ConditionsYield
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
486460-32-6

sitagliptin

Sitagliptin hydrochloride

Sitagliptin hydrochloride

Conditions
ConditionsYield
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

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