ABSTRACT: The dihydropyrimidione ring systemis contained whitin a number of pharmacologically active agents. Therefore. inrecent years, several improved prodedures for the synthesis of dihydropyrimidin-2(1H)-ones have been reported.Many of these methodes suffer from drawbacks like longer reaction times, unsatisfactory yields and cumbersome product isolation procedures. In this work, the use of acylals or acetals as aldhyde equivalents for the one-pot synthesis of dihydropyrimidin-2(1H)-ones is reported. This procedure develops the well known Bigenilli reaction while not limiting one of the substrates to being an aldehyde.
Journal of Applied Chemical Research. 01/2007;