Lipase-Catalyzed Enantioselective Synthesis of Optically Active Mephobarbital, Hexobarbital and Febarbamate

Abstract

Chiral 5, 5-disubstituted N-acyloxymethylbarbiturates have been obtained in 40-99% optical yields by lipase-catalyzed hydrolyses of 5, 5-disubstituted N, N'-bisacyloxymethylbarbiturates in H₂O-saturated diisopropyl ether. These chiral barbiturates were readily converted into chiral drugs, mephobarbital, hexobarbital and febarbamate.