WebIn an enzymatic cascade, lipase converted β-ketoester substrate to β-keto acid, which was subsequently aminated by the selected ω-TA to its corresponding β-amino acid. A potent enzyme from Ilumatobacter coccineus (ω-TAIC) was … WebNov 1, 2015 · The various enantiospecific and asymmetric syntheses of (R )-sitagliptin that have been reported over the past decade, are based on 2 major approaches: either (i) via coupling of an enantiopure β-amino acid fragment to the requisite triazolopyrazine, or (ii) via stereoselective reduction protocols. References 1
US20120108598A1 - Sitagliptin synthesis - Google Patents
WebJan 9, 2024 · Sitagliptin, a chiral β-amino acid derivative, is the active ingredient in Januvia TM. Merck used a first-generation synthesis of sitagliptin to prepare over 200 pounds for clinical trials. With modifications, this synthesis could have been a viable manufacturing process, but it required eight steps including a number of aqueous work-ups. WebPromoter engineering-mediated Tuning of esterase and transaminase expression for the chemoenzymatic synthesis of sitagliptin phosphate at the kilogram-scale ... (100-300 mM) resulted in excellent conversions of 82%-95% for the desired product. Finally, a kilogram-scale enzymatic reaction (250 mM substrate, 220 L) was carried out to produce β ... building \u0026 physical premises safety
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Webharness the reactivity of enzymatic catalysts in the context of living organisms to produce molecules directly from fermen-tations.[3,4] While organic chemists have been increasingly utilizing enzymes in synthetic efforts[5] such as the industrial-scale synthesis of the diabetes drug sitagliptin (Januvia),[6] Webasymmetric synthesis in a pilot-scale production. Besides, recently, several synthesis methods of sitagliptin have been reported on laboratory scale, including biocatalytic … Webthe enzymatic synthesis of sitagliptin, the R-selective TA derived from Arthrobacter sp. was recently engineered using computational modeling and iterative directed evolution tools. building \u0026 other construction workers act