One-pot synthesis of dihydropyrimidones using silica-supported heteropoly acid as an efficient and reusable catalyst: Improved protocol conditions for the Biginelli reaction

An efficient synthesis of 3,4-dihydropyrimidinones or thiones (DHPMs) is described, using silica-supported heteropoly acid H3PW12O40/SiO2 (PW/SiO2) for the first time as the catalyst from an aldehyde, β-keto ester and urea or thiourea in acetonitrile. Compared to the classical Biginelli reaction conditions, this method consistently has the advantage of excellent yields, mild reaction conditions, ease of workup, survival of different functional groups, and short reaction times.

One-pot synthesis of dihydropyrimidones catalyzed by silica-supported heteropoly acid as an efficient, inexpensive, easily available, and reusable catalyst. Mild reaction conditions, ease of workup, high yields, and short reaction times are features of this new procedure.Figure optionsDownload as PowerPoint slide