发明名称 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.
申请公布号 EP1775347(A2) 申请公布日期 2007.04.18
申请号 EP20060021182 申请日期 2006.10.09
申请人 PROCOS S.P.A. 发明人 BERTOLINI, GIORGIO;BOGOGNA, LUIGI;PREGNOLATO, MASSIMO;TERRENI, MARCO;VELARDI, FRANCESCO
分类号 C12P17/10;C12P41/00 主分类号 C12P17/10
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