Since thalidomide shock, it has been recognized that the enantiomers of chi
ral medicines have the different pharmacological activities, and many chemi
sts have tried to synthesize such medicines in an optically pure form. But
most of them were developed and used in clinics as racemates so far. 4-Aryl
-1,4-dihydropyridine-3,5-dicarboxylic diesters as one example have been use
d for treatment of cardiovascular disease, and are important compounds whic
h had about 85% share of calcium antagonists in 1995 in Japan. We have inve
stigated the asymmetric synthesis of these derivatives. In view of the impo
rtance of chirality to pharmacological activity, the present article descri
bes the methods of the lipase-catalyzed resolution and asymmetric synthesis
of 1-aryl-1,4-dihydropyridine-3,5-dicarboxylic diesters.