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

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...

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Bibliographic Details
Published in:	Synthetic communications Vol. 37; no. 19; pp. 3439 - 3446
Main Authors:	Vankawala, Pravinchandra J., Kolla, Naveenkumar, Elati, Chandrashekar R., Sreenivasulu, M., Kumar, K. Arun, Anjaneyulu, Yerrimilli, Venkatraman, Sundaram, Bhattacharya, Apurba, Mathad, Vijayavitthal T.
Format:	Journal Article
Language:	English
Published:	Taylor & Francis Group 01-09-2007
Subjects:	aprepitant Candida antarctica lipase-B (CAL-B) economic synthesis enantioselctive transesterification
Online Access:	Get full text
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Summary:	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.
ISSN:	0039-7911 1532-2432
DOI:	10.1080/00397910701487473