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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 ap

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:1 Kilogram

FOB Price: $5.0 / 10.0

Type:Manufacturers

inquiry

Chemwill Asia Co., Ltd.

Our main production base is located in Xuzhou industry park. We are certified both to the ISO 9001 and ISO 14001 Standards, have a safety management system in place.Our R&D team masters core technology for process-design of target building block

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:5 Kiloliter

FOB Price: $1.2 / 5.0

Type:Manufacturers

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

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:1 Kilogram

FOB Price: $9.0 / 99.0

Type:Trading Company

inquiry

Hebei Sankai Chemical Technology Co., Ltd

1. Product advantages High purity, all above 98.5%, no impurities after dissolution We will test each batch to ensure quality OEM and private brand services designed for free Various cap colors available We can also provide MT1 peptide powd

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:1 Kilogram

FOB Price: $8.0 / 20.0

Type:Trading Company

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

Saxagliptin Hydrochloride Manufacturer For Saxagliptin Intermediate

Cas:709031-78-7

Min.Order:10 Gram

Negotiable

Type:Other

inquiry

Dayang Chem (Hangzhou) Co.,Ltd.

As a leading manufacturer and supplier of chemicals in China, DayangChem not only supply popular chemicals, but also DayangChem’s R&D center offer custom synthesis according to the contract research and development services for the fine chemicals, ph

Saxagliptin hydrochloride (anhydrous)

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Qingdao Beluga Import and Export Co., LTD

Saxagliptin hydrochloride CAS:709031-78-7 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 organ

Saxagliptin hydrochloride CAS:709031-78-7

Cas:709031-78-7

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Wuhan Wonda Pharm Limited

1.high quality: quality is life. quality is the most important element for all goods. we have a lab doing research in wuhan china. hplc and nmr is available if needed. 2.reasonable price: we provide high quality products wi

high quality Saxagliptin hydrochloride/Saxagliptin HCL 99% CAS 709031-78-7

Cas:709031-78-7

Min.Order:10 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Henan Wentao Chemical Product Co., Ltd.

Henan Wentao Chemical Product Co.,Ltd is Located in Zhengzhou High-tech Development Zone with import and export license, We passed ISO 9001:2008 as well, Henan Wentao has developed more than 1000 compounds, which are widely used in the fields of prod

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Xiamen Hisunny Chemical Co.,Ltd

Best quality & Attractive price & Professional service; Trial & Pilot & Commercial Hisunny Chemical is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality intermediates, specia

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Manufacturers

inquiry

Triumph International Development Limilted

Appearance:white or light yellow crystalline powder Storage:Store in a cool,dry place and keep away from direct strong light Package:As customer request Application:Used for research and industrial manufacture. Transportation:As

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:100 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Taizhou Crene Biotechnology co.ltd

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-

Saxagliptin HCL 709031-78-7

Cas:709031-78-7

Min.Order:100 Milligram

Negotiable

Type:Lab/Research institutions

inquiry

Afine Chemicals Limited

Our Services 1. New Molecules R&D 2. Own test center HPLC NMR GC LC-MS 3. API and Intermediates from China reputed manufacturers 4. Documents support COA MOA MSDS DMF open part Our advantages 1. Government awarded company. Top 100 enter

SAXAGLIPTIN HCL

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Zibo Hangyu Biotechnology Development Co., Ltd

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

Saxagliptin hydrochloride CAS NO.709031-78-7

Cas:709031-78-7

Min.Order:10 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Hangzhou Lingrui Chemical Co.,Ltd.

High purity Saxagliptin hydrochloride 709031-78-7 in stock immediately delivery good supplierAppearance:Powder Storage:Dry and ventilated Package:according to customers' requirements Application:APIs Transportation:By air(EMS or EUB or FedEx or TNT e

HANGZHOU YUNUO CHEMICAL CO.,LTD

Superior quality, moderate price & quick delivery. Appearance:white crystalline powder Storage:Stored in cool, dry and ventilation place; Away from fire and heat Package:1kg/bag, 1kg/drum or 25kg/drum or as per your request. Application:Used as

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:1 Kilogram

Negotiable

Type:Trading Company

inquiry

Zibo Dorne chemical technology co. LTD

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,

Saxagliptin HCL salt

Cas:709031-78-7

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Xiamen Jenny Chemical Technology Co., Ltd.

GMP 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,

Saxagliptinhydrochloride

Cas:709031-78-7

Min.Order:1 Milligram

Negotiable

Type:Trading Company

inquiry

Hangzhou Huarong Pharm Co., Ltd.

We Huarong Pharm can provide Customized Synthesis & Process R&D & APIs and intermediates Production & Quality Research & Registration Application, especially our GMP validation service which complies with SFDA, FDA, WHO and EU EMPA. O

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Trading Company

inquiry

Shandong Mopai Biotechnology Co., LTD

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

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Hangzhou Zhongqi chem Co.,Ltd.

Located in Hangzhou National Hi-Tech Industrial Development Zone, zhongqichem is a technical company mainly focus on the Custom synthesis, manufacturing, sales of chemicals to various industries. Benefiting from the outstanding customer service an

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:1 Gram

Negotiable

Type:Other

inquiry

Suzhou Health Chemicals Co., Ltd.

High quality,stable supply chain.Appearance:white/off-white or light yellow Storage:Store in cool and dry place, keep away from strong light and heat. Package:aluminum bottle,glass bottle,PTFE bottle,cardboard drum Application:Active Pharmaceutical I

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Bluecrystal chem-union

We 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

GIHI CHEMICALS CO.,LIMITED

Lower price, sample is available,SDS test documents are available,large stock in warehouseAppearance:White powder Storage:Sealed and preserved Package:200/Kilograms Application:Fine chemical intermediates, used as the main raw material for the synthe

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Hangzhou Dingyan Chem Co., Ltd

manufacture Application:The refence standard products, for lab use, also we could produce bigger quantity on yr requirement.

saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Henan Allgreen Chemical Co.,Ltd

high quality Storage:Sealed, dry, microtherm , avoid light and smell. Package:According to the demand of customer Application:Organic synthesis Transportation:by air or by sea

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Manufacturers

inquiry

Hubei Taiho Chemical Co.,LTD

TAIHO Unique Advantages:1.We're factory2.Free samples available3.Commodity inspection can be done4.ISO9001,Kosher certifications5.10 years experiences Storage:Store in cool &dry place Package:aluminium foil bag/fiber can/plastic drum Application:comp

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Manufacturers

inquiry

Koning Pharmchem Co., Ltd.

KONING PHARMCHEM CO., LTD. has committed itself to a strategy of providing a unique service for companies involved in the manufacture of pharmaceuticals, healthcare products, food, cosmetics and other fine chemicals. Our products including but not li

Saxagliptin Hcl

Cas:709031-78-7

Min.Order:0

Negotiable

Type:Trading Company

inquiry

BOC Sciences

BOC Sciences provides a wide range of research chemicals and biochemicals including inhibitors, building blocks, GMP Products, impurities and metabolites, APIs for Veterinary, Natural Compounds, ADCs, Stem Cell Molecule and chiral compounds. https:

Saxagliptin hydrochloride

Cas:709031-78-7

Min.Order:1 Gram

Negotiable

Type:Trading Company

inquiry

Hangzhou JINLAN Pharm-Drugs Technology Co., Ltd

Specification:USP/EP Month production ablity:50kg/Month Low price& High quality Manufacturer Appearance:white powder Storage:Room Temperature Application:709031-78-7

Saxagliptin Hydrochloride

Cas:709031-78-7

Min.Order:0 Metric Ton

Negotiable

Type:Trading Company

inquiry

Synthetic route

saxagliptin

saxagliptin

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
With hydrogenchloride In water; ethyl acetate at 5 - 10℃;99%
With chloro-trimethyl-silane In acetone for 1h;
Multi-step reaction with 2 steps
1: 20 - 30 °C
2: hydrogenchloride; water / acetone / 1.25 h
View Scheme
(1S,3S,5S)-2-[(2S)-2-tritylamino-2-(3-hydroxyadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile

(1S,3S,5S)-2-[(2S)-2-tritylamino-2-(3-hydroxyadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
With hydrogenchloride; water In methanol at 25℃; for 3h;90%
C25H31N3O2

C25H31N3O2

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Stage #1: C25H31N3O2 With palladium 10% on activated carbon In methanol at 25 - 30℃; for 2h;
Stage #2: With hydrogenchloride In ethyl acetate at 25 - 30℃; for 4h;
80%
Stage #1: C25H31N3O2 With palladium 10% on activated carbon In methanol at 25 - 30℃; for 2h;
Stage #2: With hydrogenchloride In water; ethyl acetate at 25 - 30℃; for 4h;
80%
C18H23N5O2

C18H23N5O2

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Stage #1: C18H23N5O2 With ammonium chloride; zinc In methanol; water at 25 - 30℃; for 2h;
Stage #2: With hydrogenchloride In water at 25 - 30℃; for 4h;
73%
Stage #1: C18H23N5O2 With ammonium chloride; zinc In methanol; water at 25 - 30℃; for 2h;
Stage #2: With hydrogenchloride In water; ethyl acetate at 25 - 30℃; for 4h;
73%
saxagliptin monohydrochloride dihydrate

saxagliptin monohydrochloride dihydrate

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
In ethanol at 45℃;
3-cyano-(αS)-α-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)-β-oxo-(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-2-ethanecarbamic acid 1,1-dimethylethyl ester
709031-43-6

3-cyano-(αS)-α-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)-β-oxo-(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-2-ethanecarbamic acid 1,1-dimethylethyl ester

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: hydrogenchloride / isopropyl alcohol; water / 2.08 h / 20 - 65 °C
2: 20 - 30 °C
3: hydrogenchloride; water / acetone / 1.25 h
View Scheme
With hydrogenchloride In propan-1-ol; water Product distribution / selectivity; Reflux;
With hydrogenchloride; water In isopropyl alcohol at 20 - 65℃; for 1h;50 g
With dichloromethane In methanol at 20℃; Inert atmosphere;
tert-butyl [(1S)-2-[(1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hex-2-yl]-1-(3-hydroxytricyclo[3.3.1.13'7]dec-1-yl)-2-oxoethyl]carbamate
361442-01-5

tert-butyl [(1S)-2-[(1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hex-2-yl]-1-(3-hydroxytricyclo[3.3.1.13'7]dec-1-yl)-2-oxoethyl]carbamate

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: triethylamine / dichloromethane / 0.5 h / 0 °C
1.2: 0.58 h / 0 - 7 °C
2.1: hydrogenchloride / isopropyl alcohol; water / 2.08 h / 20 - 65 °C
3.1: 20 - 30 °C
4.1: hydrogenchloride; water / acetone / 1.25 h
View Scheme
Multi-step reaction with 2 steps
1: triethylamine; trifluoroacetyl chloride / dichloromethane / 0 - 10 °C
2: hydrogenchloride / water; propan-1-ol / Reflux
View Scheme
Multi-step reaction with 2 steps
1.1: pyridine; trifluoroacetic anhydride / 0.5 h / Cooling with ice
1.2: 7.55 h / Cooling
2.1: dichloromethane / methanol / 20 °C / Inert atmosphere
View Scheme
(1S,3S,5S)-2-[(2S)-2-propan-2-ylideneamino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]-hexane-3-carbonitrile
1346445-79-1

(1S,3S,5S)-2-[(2S)-2-propan-2-ylideneamino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]-hexane-3-carbonitrile

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
With hydrogenchloride; water In acetone for 1.25h;
With ammonium chloride at 20℃; pH=4.53;
(S)-3-hydroxyadamantylglycine-L-cis-4,5-methanoprolinenitrile TFA salt
361442-05-9

(S)-3-hydroxyadamantylglycine-L-cis-4,5-methanoprolinenitrile TFA salt

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Stage #1: (S)-3-hydroxyadamantylglycine-L-cis-4,5-methanoprolinenitrile TFA salt With sodium hydroxide In water
Stage #2: With hydrogenchloride In dichloromethane; water
benzyl N-[(1S)-2-[(1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hexan-2-yl]-1-(3-hydroxyadamantan-1-yl)-2-oxoethyl]carbamate

benzyl N-[(1S)-2-[(1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hexan-2-yl]-1-(3-hydroxyadamantan-1-yl)-2-oxoethyl]carbamate

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: trifluoroacetic anhydride; 3-pyridinecarboxylic acid ethyl ester / ethyl acetate / 6 h / 0 - 5 °C
1.2: 2 h / 25 °C
2.1: 5%-palladium/activated carbon; hydrogen / acetonitrile / 4 h / 20 - 25 °C
3.1: hydrogenchloride / water; ethyl acetate / 5 - 10 °C
View Scheme
benzyl N-[(1S)-2-[(1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl]-1-(3-hydroxyadamantan-1-yl)-2-oxoethyl]carbamate

benzyl N-[(1S)-2-[(1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl]-1-(3-hydroxyadamantan-1-yl)-2-oxoethyl]carbamate

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 5%-palladium/activated carbon; hydrogen / acetonitrile / 4 h / 20 - 25 °C
2: hydrogenchloride / water; ethyl acetate / 5 - 10 °C
View Scheme
(2S)-2-{[(benzyloxy)carbonyl]amino}-2-(3-hydroxyadamantan-1-yl)acetic acid

(2S)-2-{[(benzyloxy)carbonyl]amino}-2-(3-hydroxyadamantan-1-yl)acetic acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / ethyl acetate; acetonitrile / 8.25 h / 20 °C
2: 5%-palladium/activated carbon; hydrogen / acetonitrile / 4 h / 20 - 25 °C
3: hydrogenchloride / water; ethyl acetate / 5 - 10 °C
View Scheme
Multi-step reaction with 4 steps
1.1: N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 4.25 h / 20 °C
2.1: trifluoroacetic anhydride; 3-pyridinecarboxylic acid ethyl ester / ethyl acetate / 6 h / 0 - 5 °C
2.2: 2 h / 25 °C
3.1: 5%-palladium/activated carbon; hydrogen / acetonitrile / 4 h / 20 - 25 °C
4.1: hydrogenchloride / water; ethyl acetate / 5 - 10 °C
View Scheme
(1S)-α-amino-3-hydroxyadamantane-acetic acid hydrochloride
865999-64-0

(1S)-α-amino-3-hydroxyadamantane-acetic acid hydrochloride

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: sodium hydroxide / water / 4 h / 25 - 30 °C / pH 8.5 - 9.5
2: N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / ethyl acetate; acetonitrile / 8.25 h / 20 °C
3: 5%-palladium/activated carbon; hydrogen / acetonitrile / 4 h / 20 - 25 °C
4: hydrogenchloride / water; ethyl acetate / 5 - 10 °C
View Scheme
Multi-step reaction with 5 steps
1.1: sodium hydroxide / water / 4 h / 25 - 30 °C / pH 8.5 - 9.5
2.1: N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 4.25 h / 20 °C
3.1: trifluoroacetic anhydride; 3-pyridinecarboxylic acid ethyl ester / ethyl acetate / 6 h / 0 - 5 °C
3.2: 2 h / 25 °C
4.1: 5%-palladium/activated carbon; hydrogen / acetonitrile / 4 h / 20 - 25 °C
5.1: hydrogenchloride / water; ethyl acetate / 5 - 10 °C
View Scheme
Multi-step reaction with 4 steps
1.1: triethylamine / dichloromethane / 4 h / 15 - 35 °C
2.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 12 h / 5 - 35 °C
3.1: pyridine; trifluoroacetic anhydride / tetrahydrofuran / 3.5 h / 0 - 10 °C
3.2: 3.5 h / 25 °C / pH 10 - 11
4.1: water; hydrogenchloride / methanol / 3 h / 25 °C
View Scheme
(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carbonitrile 4-methylbenzenesulfonate
929106-57-0

(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carbonitrile 4-methylbenzenesulfonate

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / ethyl acetate; acetonitrile / 8.25 h / 20 °C
2: 5%-palladium/activated carbon; hydrogen / acetonitrile / 4 h / 20 - 25 °C
3: hydrogenchloride / water; ethyl acetate / 5 - 10 °C
View Scheme
(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide

(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 4.25 h / 20 °C
2.1: trifluoroacetic anhydride; 3-pyridinecarboxylic acid ethyl ester / ethyl acetate / 6 h / 0 - 5 °C
2.2: 2 h / 25 °C
3.1: 5%-palladium/activated carbon; hydrogen / acetonitrile / 4 h / 20 - 25 °C
4.1: hydrogenchloride / water; ethyl acetate / 5 - 10 °C
View Scheme
C12H17N3O3

C12H17N3O3

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: benzotriazol-1-ol / ethyl acetate; acetonitrile / 0.17 h / 25 - 30 °C / Inert atmosphere
1.2: 0.17 h / 25 - 30 °C
1.3: 0 - 30 °C / Inert atmosphere
2.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
2.2: 3 h / 25 - 45 °C
3.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
3.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 4 steps
1.1: (S)-1-phenyl-ethylamine / acetone / 7 h / 25 - 65 °C
2.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
2.2: 4 h / 0 - 20 °C
3.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
3.2: 3 h / 25 - 45 °C
4.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
4.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 4 steps
1.1: (S)-1-phenyl-ethylamine / acetone / 7 h / 25 - 65 °C
1.2: 2 h / 25 - 30 °C
2.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
3.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
3.2: 3 h / 25 - 45 °C
4.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
4.2: 4 h / 25 - 30 °C
View Scheme
C12H17N3O3

C12H17N3O3

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
1.2: 4 h / 0 - 20 °C
2.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
2.2: 3 h / 25 - 45 °C
3.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
3.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 3 steps
1.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
2.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
2.2: 3 h / 25 - 45 °C
3.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
3.2: 4 h / 25 - 30 °C
View Scheme
C18H25N5O3

C18H25N5O3

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
1.2: 3 h / 25 - 45 °C
2.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
2.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 2 steps
1.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
1.2: 3 h / 25 - 45 °C
2.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
2.2: 4 h / 25 - 30 °C
View Scheme
C19H25NO3

C19H25NO3

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: (S)-1-phenyl-ethylamine / methanol / 7 h / 25 - 65 °C
2.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
2.2: 4 h / 0 - 20 °C
3.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
3.2: 3 h / 25 - 45 °C
4.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
4.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 4 steps
1.1: (S)-1-phenyl-ethylamine / methanol / 7 h / 25 - 65 °C
1.2: 1 h / 25 - 30 °C
2.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
3.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
3.2: 3 h / 25 - 45 °C
4.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
4.2: 4 h / 25 - 30 °C
View Scheme
C19H25NO3

C19H25NO3

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
1.2: 4 h / 0 - 20 °C
2.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
2.2: 3 h / 25 - 45 °C
3.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
3.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 3 steps
1.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
2.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
2.2: 3 h / 25 - 45 °C
3.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
3.2: 4 h / 25 - 30 °C
View Scheme
C25H33N3O3

C25H33N3O3

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
1.2: 3 h / 25 - 45 °C
2.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
2.2: 4 h / 25 - 30 °C
View Scheme
(adamant-1-yl)-acetic acid
4942-47-6

(adamant-1-yl)-acetic acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: thionyl chloride / 1.5 h / 20 °C / Inert atmosphere
1.2: 3 h / 25 - 75 °C
2.1: sulfuric acid; nitric acid / water / 0 - 10 °C
3.1: tetrabutylammomium bromide; sodium azide / water; toluene / 25 - 80 °C
4.1: benzotriazol-1-ol / ethyl acetate; acetonitrile / 0.17 h / 25 - 30 °C / Inert atmosphere
4.2: 0.17 h / 25 - 30 °C
4.3: 0 - 30 °C / Inert atmosphere
5.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
5.2: 3 h / 25 - 45 °C
6.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
6.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 7 steps
1.1: thionyl chloride / 1.5 h / 20 °C / Inert atmosphere
1.2: 3 h / 25 - 75 °C
2.1: sulfuric acid; nitric acid / water / 0 - 10 °C
3.1: tetrabutylammomium bromide; sodium azide / water; toluene / 25 - 80 °C
4.1: (S)-1-phenyl-ethylamine / acetone / 7 h / 25 - 65 °C
5.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
5.2: 4 h / 0 - 20 °C
6.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
6.2: 3 h / 25 - 45 °C
7.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
7.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 7 steps
1.1: thionyl chloride / 1.5 h / 20 °C / Inert atmosphere
1.2: 3 h / 25 - 75 °C
2.1: sulfuric acid; nitric acid / water / 0 - 10 °C
3.1: 3 h / 110 °C
4.1: (S)-1-phenyl-ethylamine / methanol / 7 h / 25 - 65 °C
5.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
5.2: 4 h / 0 - 20 °C
6.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
6.2: 3 h / 25 - 45 °C
7.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
7.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 7 steps
1.1: thionyl chloride / 1.5 h / 20 °C / Inert atmosphere
1.2: 3 h / 25 - 75 °C
1.3: 3 h / 0 - 75 °C
2.1: sulfuric acid; nitric acid / 0 - 10 °C
2.2: 2 h / 0 - 10 °C
3.1: 3 h / 110 °C
4.1: (S)-1-phenyl-ethylamine / methanol / 7 h / 25 - 65 °C
4.2: 1 h / 25 - 30 °C
5.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
6.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
6.2: 3 h / 25 - 45 °C
7.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
7.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 7 steps
1.1: thionyl chloride / 1.5 h / 20 °C / Inert atmosphere
1.2: 3 h / 25 - 75 °C
1.3: 3 h / 0 - 75 °C
2.1: sulfuric acid; nitric acid / 0 - 10 °C
2.2: 2 h / 0 - 10 °C
3.1: tetrabutylammomium bromide; sodium azide / toluene; water / 25 - 80 °C
4.1: (S)-1-phenyl-ethylamine / acetone / 7 h / 25 - 65 °C
4.2: 2 h / 25 - 30 °C
5.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
6.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
6.2: 3 h / 25 - 45 °C
7.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
7.2: 4 h / 25 - 30 °C
View Scheme
2-(1-adamantyl)-2-bromoacetic acid
59768-70-6

2-(1-adamantyl)-2-bromoacetic acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: sulfuric acid; nitric acid / water / 0 - 10 °C
2.1: tetrabutylammomium bromide; sodium azide / water; toluene / 25 - 80 °C
3.1: benzotriazol-1-ol / ethyl acetate; acetonitrile / 0.17 h / 25 - 30 °C / Inert atmosphere
3.2: 0.17 h / 25 - 30 °C
3.3: 0 - 30 °C / Inert atmosphere
4.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
4.2: 3 h / 25 - 45 °C
5.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
5.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 6 steps
1.1: sulfuric acid; nitric acid / water / 0 - 10 °C
2.1: tetrabutylammomium bromide; sodium azide / water; toluene / 25 - 80 °C
3.1: (S)-1-phenyl-ethylamine / acetone / 7 h / 25 - 65 °C
4.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
4.2: 4 h / 0 - 20 °C
5.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
5.2: 3 h / 25 - 45 °C
6.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
6.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 6 steps
1.1: sulfuric acid; nitric acid / water / 0 - 10 °C
2.1: 3 h / 110 °C
3.1: (S)-1-phenyl-ethylamine / methanol / 7 h / 25 - 65 °C
4.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
4.2: 4 h / 0 - 20 °C
5.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
5.2: 3 h / 25 - 45 °C
6.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
6.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 6 steps
1.1: sulfuric acid; nitric acid / 0 - 10 °C
1.2: 2 h / 0 - 10 °C
2.1: 3 h / 110 °C
3.1: (S)-1-phenyl-ethylamine / methanol / 7 h / 25 - 65 °C
3.2: 1 h / 25 - 30 °C
4.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
5.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
5.2: 3 h / 25 - 45 °C
6.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
6.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 6 steps
1.1: sulfuric acid; nitric acid / 0 - 10 °C
1.2: 2 h / 0 - 10 °C
2.1: tetrabutylammomium bromide; sodium azide / toluene; water / 25 - 80 °C
3.1: (S)-1-phenyl-ethylamine / acetone / 7 h / 25 - 65 °C
3.2: 2 h / 25 - 30 °C
4.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
5.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
5.2: 3 h / 25 - 45 °C
6.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
6.2: 4 h / 25 - 30 °C
View Scheme
α-bromo-3-hydroxy-1-adamantyl acetic acid

α-bromo-3-hydroxy-1-adamantyl acetic acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: tetrabutylammomium bromide; sodium azide / water; toluene / 25 - 80 °C
2.1: benzotriazol-1-ol / ethyl acetate; acetonitrile / 0.17 h / 25 - 30 °C / Inert atmosphere
2.2: 0.17 h / 25 - 30 °C
2.3: 0 - 30 °C / Inert atmosphere
3.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
3.2: 3 h / 25 - 45 °C
4.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
4.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 5 steps
1.1: tetrabutylammomium bromide; sodium azide / water; toluene / 25 - 80 °C
2.1: (S)-1-phenyl-ethylamine / acetone / 7 h / 25 - 65 °C
3.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
3.2: 4 h / 0 - 20 °C
4.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
4.2: 3 h / 25 - 45 °C
5.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
5.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 5 steps
1.1: 3 h / 110 °C
2.1: (S)-1-phenyl-ethylamine / methanol / 7 h / 25 - 65 °C
3.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / ethyl acetate; acetonitrile / 0.25 h / 20 °C
3.2: 4 h / 0 - 20 °C
4.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
4.2: 3 h / 25 - 45 °C
5.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
5.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 5 steps
1.1: tetrabutylammomium bromide; sodium azide / toluene; water / 25 - 80 °C
2.1: (S)-1-phenyl-ethylamine / acetone / 7 h / 25 - 65 °C
2.2: 2 h / 25 - 30 °C
3.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
4.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
4.2: 3 h / 25 - 45 °C
5.1: zinc; ammonium chloride / water; methanol / 2 h / 25 - 30 °C
5.2: 4 h / 25 - 30 °C
View Scheme
Multi-step reaction with 5 steps
1.1: 3 h / 110 °C
2.1: (S)-1-phenyl-ethylamine / methanol / 7 h / 25 - 65 °C
2.2: 1 h / 25 - 30 °C
3.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / acetonitrile; ethyl acetate / 4 h / 0 - 20 °C
4.1: pyridine; trifluoroacetic anhydride / ethyl acetate / 0 - 5 °C
4.2: 3 h / 25 - 45 °C
5.1: palladium 10% on activated carbon / methanol / 2 h / 25 - 30 °C
5.2: 4 h / 25 - 30 °C
View Scheme
(αS)-α-[[(1,1-dimethylethoxy)carbonyl]-amino]-3-hydroxytricyclo[3.3.1.13,7]decane-1-acetic acid
361442-00-4

(αS)-α-[[(1,1-dimethylethoxy)carbonyl]-amino]-3-hydroxytricyclo[3.3.1.13,7]decane-1-acetic acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: hydrogenchloride / isopropyl alcohol; dichloromethane / 8 h / 10 - 35 °C
2.1: triethylamine / dichloromethane / 4 h / 15 - 35 °C
3.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 12 h / 5 - 35 °C
4.1: pyridine; trifluoroacetic anhydride / tetrahydrofuran / 3.5 h / 0 - 10 °C
4.2: 3.5 h / 25 °C / pH 10 - 11
5.1: water; hydrogenchloride / methanol / 3 h / 25 °C
View Scheme
Multi-step reaction with 3 steps
1.1: methanesulfonyl chloride; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / Cooling with acetone-dry ice
1.2: 20 °C
2.1: pyridine; trifluoroacetic anhydride / 0.5 h / Cooling with ice
2.2: 7.55 h / Cooling
3.1: dichloromethane / methanol / 20 °C / Inert atmosphere
View Scheme
(1S)-1-[triphenylmethylamino]-3-hydroxyadamantane-1-acetic acid

(1S)-1-[triphenylmethylamino]-3-hydroxyadamantane-1-acetic acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 12 h / 5 - 35 °C
2.1: pyridine; trifluoroacetic anhydride / tetrahydrofuran / 3.5 h / 0 - 10 °C
2.2: 3.5 h / 25 °C / pH 10 - 11
3.1: water; hydrogenchloride / methanol / 3 h / 25 °C
View Scheme
[1S-(1α,3β,5α)]-3-(aminocarbonyl)-2-azabicyclo[3.1.0]hexane-2-carboxylic acid 1,1-dimethylethyl ester
361440-67-7

[1S-(1α,3β,5α)]-3-(aminocarbonyl)-2-azabicyclo[3.1.0]hexane-2-carboxylic acid 1,1-dimethylethyl ester

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: isopropyl alcohol / 5 h / 60 - 70 °C
2.1: dichloromethane / 0.25 h / 25 - 35 °C
2.2: 13.25 h / 5 - 35 °C
3.1: pyridine; trifluoroacetic anhydride / tetrahydrofuran / 3.5 h / 0 - 10 °C
3.2: 3.5 h / 25 °C / pH 10 - 11
4.1: water; hydrogenchloride / methanol / 3 h / 25 °C
View Scheme
Multi-step reaction with 4 steps
1.1: isopropyl alcohol / 5 h / 60 - 70 °C
2.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 12 h / 5 - 35 °C
3.1: pyridine; trifluoroacetic anhydride / tetrahydrofuran / 3.5 h / 0 - 10 °C
3.2: 3.5 h / 25 °C / pH 10 - 11
4.1: water; hydrogenchloride / methanol / 3 h / 25 °C
View Scheme
Multi-step reaction with 4 steps
1.1: hydrogenchloride / water; tetrahydrofuran; ethyl acetate / 18 h / 20 °C
2.1: methanesulfonyl chloride; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / Cooling with acetone-dry ice
2.2: 20 °C
3.1: pyridine; trifluoroacetic anhydride / 0.5 h / Cooling with ice
3.2: 7.55 h / Cooling
4.1: dichloromethane / methanol / 20 °C / Inert atmosphere
View Scheme
(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide methane sulphonic acid
709031-45-8

(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide methane sulphonic acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 12 h / 5 - 35 °C
2.1: pyridine; trifluoroacetic anhydride / tetrahydrofuran / 3.5 h / 0 - 10 °C
2.2: 3.5 h / 25 °C / pH 10 - 11
3.1: water; hydrogenchloride / methanol / 3 h / 25 °C
View Scheme
Multi-step reaction with 3 steps
1.1: dichloromethane / 0.25 h / 25 - 35 °C
1.2: 13.25 h / 5 - 35 °C
2.1: pyridine; trifluoroacetic anhydride / tetrahydrofuran / 3.5 h / 0 - 10 °C
2.2: 3.5 h / 25 °C / pH 10 - 11
3.1: water; hydrogenchloride / methanol / 3 h / 25 °C
View Scheme
(5S)-5-aminocarbonyl-4,5-dihydro-1H-pyrrole-1-carboxylic acid 1-(1,1-dimethylethyl) ester
709031-38-9

(5S)-5-aminocarbonyl-4,5-dihydro-1H-pyrrole-1-carboxylic acid 1-(1,1-dimethylethyl) ester

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: diethylzinc / dichloromethane; toluene; 1,2-dimethoxyethane / 0.75 h / -30 - -20 °C / Large scale
1.2: -25 - 24 °C / Large scale
2.1: hydrogenchloride / water; tetrahydrofuran; ethyl acetate / 18 h / 20 °C
3.1: methanesulfonyl chloride; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / Cooling with acetone-dry ice
3.2: 20 °C
4.1: pyridine; trifluoroacetic anhydride / 0.5 h / Cooling with ice
4.2: 7.55 h / Cooling
5.1: dichloromethane / methanol / 20 °C / Inert atmosphere
View Scheme
(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide hydrochloride

(1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide hydrochloride

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: methanesulfonyl chloride; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / Cooling with acetone-dry ice
1.2: 20 °C
2.1: pyridine; trifluoroacetic anhydride / 0.5 h / Cooling with ice
2.2: 7.55 h / Cooling
3.1: dichloromethane / methanol / 20 °C / Inert atmosphere
View Scheme
malonic acid
141-82-2

malonic acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

saxagliptin hydrochloride-malonic acid cocrystal (3:2)

saxagliptin hydrochloride-malonic acid cocrystal (3:2)

Conditions
ConditionsYield
In methanol at 20 - 25℃; for 0.75h;100%
saxagliptin

saxagliptin

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

saxagliptin hydrochloride-saxagliptin cocrystal (1:1)

saxagliptin hydrochloride-saxagliptin cocrystal (1:1)

Conditions
ConditionsYield
In isopropyl alcohol for 0.75h; Solvent;100%
Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

urea
57-13-6

urea

saxagliptin hydrochloride-urea cocrystal (1:3)

saxagliptin hydrochloride-urea cocrystal (1:3)

Conditions
ConditionsYield
In ethyl acetate at 65℃;93%
glycolic Acid
79-14-1

glycolic Acid

Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

saxagliptin hydrochloride-glycolic acid cocrystal (1:1)

saxagliptin hydrochloride-glycolic acid cocrystal (1:1)

Conditions
ConditionsYield
In 5,5-dimethyl-1,3-cyclohexadiene at 20 - 25℃;83%
Saxagliptin hydrochloride
709031-78-7

Saxagliptin hydrochloride

saxagliptin

saxagliptin

Conditions
ConditionsYield
In dichloromethane; water81%
With sodium carbonate In dichloromethane; water at 25 - 30℃; for 0.5h; pH=9 - 10;74%
With sodium carbonate In dichloromethane; water at 25 - 30℃; for 0.5h; pH=9 - 10;74%
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