Asymmetric synthesis of optically active 1,4-dihydropyridines as calcium antagonist [Review]

摘要

Since thalidomide shock, it has been recognized that the enantiomers of chiral medicines have the different pharmacological activities, and many chemists 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 used for treatment of cardiovascular disease, and are important compounds which had about 85% share of calcium antagonists in 1995 in Japan. We have investigated the asymmetric synthesis of these derivatives. In view of the importance of chirality to pharmacological activity, the present article describes the methods of the lipase-catalyzed resolution and asymmetric synthesis of 1-aryl-1,4-dihydropyridine-3,5-dicarboxylic diesters. [References: 174]