Process for the kinetic resolution of racemic alcohols having one or more stereogenic centers

摘要

Method for kinetic optical resolution of alcohols (I) with at least one stereogenic center, involves converting racemic (I) into racemic fluorinated carboxylate esters (II) using fluorinated acylating agents, and eliminating the fluoro-phase labeling of the more rapidly reacting enantiomer by lipase-catalyzed conversion of racemic (II) with alcohol. Method for kinetic optical resolution of alcohols (I) having at least one stereogenic center involves; (1) by firstly converting racemic (I) into racemic fluorinated carboxylate esters (II) using fluorinated acylating agents; (2) eliminating the fluoro-phase labeling of the more rapidly reacting enantiomer by lipase-catalyzed conversion of racemic (II) with alcohol (the slower reacting enantiomer remaining unchanged); and (3) extractive separation of the enantiomers by partitioning between organic and fluorine-containing phases.