Vanadium(III) chloride catalyzed Biginelli condensation:: solution phase library generation of dihydropyrimidin-(2H)-ones

The three component condensation of an aldehyde, a beta-keto ester and urea (thiourea) in the presence of a catalytic amount of VCl3 is disclosed for the solution phase synthesis of dihydropyrimidinones. The ease of synthesis and work-up allowed the parallel synthesis of a 48-membered library of dihydropyrimidinones quickly and efficiently in good yields. (C) 2003 Elsevier Ltd. All rights reserved.