Efficient Synthesis of (1R)??[3, 5??Bis (trifluoromethyl) phenyl] Ethanol, a Key Intermediate for Aprepitant, an NK??1 Receptor Antagonist

…, M Sreenivasulu, KA Kumar, Y Anjaneyulu…

文献索引：Vankawala, Pravinchandra J.; Kolla, Naveenkumar; Elati, Chandrashekar R.; Sreenivasulu; Kumar, K. Arun; Anjaneyulu, Yerrimilli; Venkatraman, Sundaram; Bhattacharya, Apurba; Mathad, Vijayavitthal T. Synthetic Communications, 2007 , vol. 37, # 19 p. 3439 - 3446

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被引用次数: 9

摘要

Abstract Enzyme??catalyzed efficient synthesis of (1R)??[3, 5??bis (trifluoromethyl) phenyl] ethanol (R)??(3), a key intermediate for aprepitant, via enantioselective transesterification of racemic 1??[3, 5??bis (trifluoromethyl) phenyl] ethanol (RS)??3 using vinyl acetate as the acyl donor in the presence of Candida antarctica lipase??B (CAL??B) in an overall yield of 84% with> 99% ee is described.