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A rapid and practical entry into cis-1,4-aminocyclohexanols
Authors:Fabrice Gallou  Bo Han  Manuela Seeger-Weibel  Simon Allmendinger
Institution:a Novartis Pharma AG, Chemical and Analytical Development, CH-4002 Basel, Switzerland
b Suzhou Novartis Pharma Technology Co., Ltd.;18 Tonglian Road, Riverside Industrial Park, Changshu Economic Development Zone, Changshu/Jiangsu Province 215537, China
Abstract:A selective and practical approach for the formation of cis-1,4-aminocyclohexanol was developed. The key transformation involves a one-pot imine formation/ Lewis acid-directed imine reduction and results in a highly selective attack of the reducing agent. This simple and practical method is easily amenable to large-scale synthesis.
Keywords:cis-1  4-Aminocyclohexanol  Reductive amination  Selectivity
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