Racemate resolution 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 is characterised in that (a) a racemic heteroatom-substituted amine is enantioselectively acylated in the presence of a hydrolase with an ester whose acid component bear a fluorine, nitrogen, phosphorus, oxygen or sulphur atom next to the carbonyl carbon atom; (b) the mixture of optically active heteroatom-substituted amine and optically active acylated heteroatom-substituted amine is separated in order to produce an enantiomer of the heteroatom-substituted amine; (c) the other enantiomer of the heteroatom-substituted amine is optionally extracted from the acylated heteroatom-substituted amine by amide cleavage.