A series of different analogs of 4-aryl-3,4-dihydropyrimidin-2(1H)-one have been synthesized and their biocatalytic resolution has been carried out using immobilized lipase CAL-L(A) (immobilized on accurel). The systematic one-step procedure is developed for the synthesis of optically enriched ethyl 4-aryl-6-methyl-3,4-dihydropyrimidin-2-one-5-carboxylates 8a-d and acylated ethyl 4-aryl-6-methyl-3,4-dihydropyrimidin-2-one-5-carboxylates 9a-e, 10a-e, 11b-d and 12a-e, by the enantioselective acylation of racemic ethyl 4-aryl-6-methyl-3,4-dihydropyrimidin-2-one-5-carboxylates using CAL-L(A).