Optical resolution of primary amines by enantioselective acylation with a long-chain alkoxyalkanoate or phenoxyalkanoate ester in the presence of a lipase

摘要

Process for preparing optically active primary amines comprises: (a) reacting a primary amine with a long-chain alkoxyalkanoate or phenoxyalkanoate ester (I) in the presence of a lipase; and (b) separating the enantioselectively acylated amine from the unreacted amine. Process for preparing optically active primary amines comprises: (a) reacting a primary amine with an ester of formula (I) in the presence of a lipase; and (b) separating the enantioselectively acylated amine from the unreacted amine: m = 0 or 1; R1 = 6-20C alkyl or 6- to 20-membered heteroalkyl, optionally substituted by 1-5 halogen atoms and/or an oxo group; R2 = 1-8C alkyl or phenyl; R3 = H or 1-8C alkyl. An Independent claim is also included for a process for acylating primary amines of formula (II), comprising reacting (II) with (I) in the presence of a lipase: n = 0 or 1; R4, R5 = H, 1-8C alkyl or phenyl; R6 = 1-6C alkyl or benzyl.