Preparation of an optically pure tetramine for chiral aza macrocycles (CA), includes biocatalytic resolution by acylation giving bisamido ester

摘要

The preparation of an optically pure tetramine for aza macrocycles (CA) has biocatalytic resolution of (+)-trans-cyclopentanodiamine (TC) by e.g. lipases in organic media. Thus acylation by diethyl malonate yields optically enantiopure bisamido ester and TC of configurations (R,R) and (S,S) respectively, for (+)- and (-)-TC production.