Synthesis of saxagliptin

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August undefined, 2024

Web1) Efficient synthesis of sitagliptin phosphate, a novel DPP-IV inhibitor, via a chiral aziridine intermediate. Xianhua Pan (advisor); Xiaojun Li; Wansheng Yu; Feng Liu. Tetrahedron Lett. 2013, 54 ... WebThe objective of this study was to evaluate the long-term safety and tolerability of saxagliptin 5 mg as add-on therapy to common antihyperglycemic drugs in patients aged ≥65 years and <65 years.Methods: Pooled adverse event data from three placebo-controlled trials of 76–206 weeks’ duration in older (≥65 years) and younger (<65 years) patients …

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WebSaxagliptin is a dipeptidyl peptidase-4 (DPP-4) ... Synthesis Reference. Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, … 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 company ato

An Efficient and Telescopic Process for Synthesis of Saxagliptin ...

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, WebOct 10, 2024 · An improved method with high yield and simple steps for the synthesis of 3-hydroxy-1-acetyladamantane was reported. 3-Hydroxy-1-acetyladamantane is an … WebAbstract: OBJECTIVE To explore a new synthesis method of the saxagliptin intermediate of the dipeptidyl peptidase Ⅳ( DPP-Ⅳ) inhibitor saxagliptin,N-BOC-3-hydroxy-1-adamantylglycine,to reduce the synthesis cost of saxagliptin. METHODS The synthesis used 1-adamantane carboxylic acid( 1) as the starting material. eat up my time

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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: … 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 … eat up the clockWebCo- 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 … eat up slim down recipes

"WebApplication 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 ... " - Synthesis of saxagliptin

Synthesis of saxagliptin

WO2012162507A1 - Process for preparing saxagliptin and its

WebAn improved method with high yield and simple steps for the synthesis of 3-hydroxy-1-acetyladamantane was reported. 3-Hydroxy-1-acetyladamantane is an important intermediate of Saxagliptin for type 2 diabetes mellitus (T2DM). Its synthetic method started from 1-adamantanecarboxylic acid via oxidation by sulfuric acid/nitric acid, then VHA … WebJan 11, 2014 · A facile synthesis of saxagliptin intermediate N -Boc-3-hydroxyadamantylglycine Introduction. Type 2 diabetes mellitus (T2DM) is a global …

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WebJul 29, 2024 · Today, organocatalysis is one of the most thriving research domains in contemporary organic synthesis and covers a series of classic catalytic modes … 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 …

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 …

WebFeb 15, 2014 · All eight stereoisomers of saxagliptin have been synthesized and evaluated for their inhibitory activity against DPP-IV. It was unambiguously confirmed that the configuration of saxagliptin was critical to potent inhibition of DPP-IV. Docking study was performed to elucidate the configuration-activity relationship of saxagliptin stereoisomers. WebAug 1, 2005 · The use of a chiral auxiliary to obtain enantiomerically pure Strecker products lustrated by the synthesis of saxagliptin, an oral antidiabetic drug belonging to th peptidyl peptidase 4 (DPP-IV ...

WebThe cyanopyrrolidine moiety of vildagliptin occupies the S1 pocket at the DPP-4 active site. Like saxagliptin, the nitrile group is stabilized through covalent imidate adduct formation with the hydroxyl of catalytic Ser630. The imidate nitrogen–hydrogen bonds with the side chain of Tyr547. The hydrophobic adamantyl moiety occupies the S2 pocket.

WebU.S. Pat. No. 7,214,702 discloses a process for the preparation of saxagliptin or its hydrochloride salt. The above documents disclose a process for the preparation of … company attendance sheet翻译Web1) REMOTELY RUN MED CHEM PROGRAMS /pharma consulting 2) discovered DPP4 inhibitor saxagliptin at BMS for type II diabetes, FDA2009 3) designed acylsulfonamide bcl-2 inhibitor for venetoclax ... company a\\u0026aWebsynthesis and purification, process controls, control of raw materials, container closure system and stability of saxagliptin are provided in NDA 22-350 for Onglyza® (saxagliptin) Tablets (from the same applicant as this NDA). The drug substance saxagliptin will be manufactured at the BMS facility in Sword, Ireland. eat urbanmeadowcafe.comWebJul 28, 2005 · Extension of this approach to adamantylglycine-derived inhibitors led to the discovery of highly potent inhibitors, including hydroxyadamantyl compound BMS-477118 … eatupwardfarmsWebNov 1, 2015 · The triazolopyrazine component required to complete the synthesis of (R )-sitagliptin 1 was prepared in 4 steps from chloropyrazine 9: treatment of 9 with NH 2 NH 2 … eatures outdoor sports businessWebFeb 2, 2024 · The second reason is the use of methanol for preparation of tablet solution which dissolve only LOR leaving the excipients because they do not dissolve ... B.M. Spectrophotometric methods based on charge transfer complexation reactions for the determination of saxagliptin in bulk and pharmaceutical preparation. Int. J. Biomed ... eat up weight gainWebIn one embodiment the present invention provides a process for the preparation of saxagliptin monohydrate, compound of Formula la without involving the use or formation of saxagliptin HC1 comprising reacting a trifluoroacetate (TFA) salt of saxagliptin, compound of formula Ilia with a base to form a reaction mixture containing a compound of Formula … eat v3