RESOLUTION OF RACEMATES OF PRIMARY AND SECONDARY HETEROATOM-SUBSTITUTED AMINES BY ENZYME-CATALYZED ACYLATION

摘要

A process for preparing optically active primary and secondary heteroatom-substituted amines from the corresponding racemates ischaracterised in that (a) a racemic heteroatom-substituted amine isenantioselectively acylated in the presence of a hydrolase with an esterwhose acid component bear a fluorine, nitrogen, phosphorus, oxygen or sulphuratom next to the carbonyl carbon atom; (b) the mixture ofoptically active heteroatom-substituted amine and optically active acylatedheteroatom-substituted amine is separated in order to produce anenantiomer of the heteroatom-substituted amine; (c) the other enantiomer ofthe heteroatom-substituted amine is optionally extracted fromthe acylated heteroatom-substituted amine by amide cleavage.