A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)-pyrrolidines by amidation with lipases

摘要

A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)pyrrolidines of formula (I)in which R is C1-C6 alkyl,which process comprises the reaction of the racemic amine with benzyl acetate in acetonitrile in the presence of a lipase selected from Pseudomonas cepacia, Pseudomonas fluorescens or Candida rugosa lipases, to give the corresponding 1-substituted N-(pyrrolidin-2-yl-methyl)-acetamides of formula (II), with R configuration,and the residual amine with S configuration,and, if desired, the subsequent hydrolysis of the amide to obtain the amine with R configuration.