Synthesis of saxagliptin
A mild and relatively simple way for preparation of 2-(3-hydroxy-1-adamantane)-2-oxoacetic acid (I) was reported. It was prepared from 1-adamantanecarboxylic acid (II) via sulfuric acid/nitric acid to get 3-hydroxy-1-adamantanecarboxylic acid (III); treated with the one-pot method through acylation, condensation, … See more Diabetes, a complex and chronic illness, is becoming a public health problem and even a global societal catastrophe. According to the … See more On account of the above hypothesis, we made some improvements based on our laboratory previous work [ 1. J. Li, S. Zhang, H. Zhou, J. Peng, Y. Feng, and X. Hu, “Preparation of 2 … See more This study provides a simple and economical method to synthesis 2-(3-hydroxy-1-adamantane)-2-oxoacetic acid in 60% yield from 1-adamantanecarboxylic acid over five steps. The reaction is mild, simple, and … See more All reagents were purchased commercially and were used as supplied unless otherwise specified. Melting points were determined through SGW X-4 micromelting point … See more WebCo- synthesis of saxagliptin hydrochloride 1 that operation from the colleagues of analytical research has following advantages over the repor ted & development department and process research & processes; (i) usage of hazardous reagents such development department of active pharmaceutical as trifluoroacetic anhydride (TFAA), phosphorous …
Synthesis of saxagliptin
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WebThe scope of adamantane and imine reaction partners is broad and deprotection provides versatile amine and amino acid building blocks. Using readily available chiral imines, the enantioselective synthesis of the saxagliptin core and rimantadine derivatives is … WebThe synthesis of intermediate 81 began from adamantine carboxylic acid methyl ester 77.Reduction to the aldehyde and its condensation with (R)-2-phenylglycinol and KCN provided compound 78.Compound 80 was obtained from 78 following acid hydrolysis, hydrogenation-mediated removal of the chiral auxiliary, and Boc protection. Hydroxylation …
WebNov 19, 2013 · Furthermore, the invention provides a method for catalytic synthesis of a saxagliptin chiral intermediate, namely (S)-N-t-butyloxycarbonyl-3-hydroxy-1-adamantyl-D … WebJun 4, 2007 · The non‐proteinogenic amino acid 2‐(3‐hydroxy‐1‐adamantyl)‐(2S)‐aminoethanoic acid (2, (S)‐3‐hydroxyadamantylglycine), is a key intermediate required for the synthesis of Saxagliptin, a dipeptidyl peptidase IV inhibitor under development for treatment of type 2 diabetes mellitus. Keto acid …
WebThe commercial-scale synthesis of the DPP-IV inhibitor, saxagliptin (1), is described from the two unnatural amino acid derivatives 2 and 3. After the deprotection of 3, the core of 1 … WebJun 4, 2007 · The non-proteinogenic amino acid 2-(3-hydroxy-1-adamantyl)-(2S)-aminoethanoic acid [2, (S)-3-hydroxyadamantylglycine], is a key intermediate required for …
WebAn efficient and telescopic process for the preparation of saxagliptin hydrochloride (1) is described using T3P as a reagent for condensation and dehydration steps. Key words: Saxagliptin; dipeptidyl peptidase-4 inhibitor; propylphosphonic anhydride (T3P) action, relatively low risk for drug-drug interactions,
WebMay 31, 2012 · DOI: 10.2174/157017812801264755 Corpus ID: 101172596; Preparation of 2-(3-Hydroxy-1-Adamantyl)-2-Oxoacetic Acid: A Key Intermediate for Saxagliptin @article{Li2012PreparationO2, title={Preparation of 2-(3-Hydroxy-1-Adamantyl)-2-Oxoacetic Acid: A Key Intermediate for Saxagliptin}, author={Jingke Li and Shurong Zhang and … chinese almond cookies recipe bestWebApplication In Synthesis of [ 361442-04-8 ] ... (40mbar, 20°C) and 10.6g Saxagliptin was isolated containing small amounts of pyridine. The white solid was dissolved in 50mL toluene and the solvent was removed via distillation (20mbar/30°) leading to 10.4g Saxagliptin (33.0mmol/74%) as white amorphous solid ... grand cayman local restaurantsWebJun 4, 2007 · The (S)-3-hydroxyadamantylglycine, a key chiral intermediate for the synthesis of saxagliptin, an inhibitor of dipeptidyl peptidase-4, and an antidiabetic drug, was synthesized by using a modified ... chinese alpha film series