Efficient Conversion of Biginelli 3,4-Dihydropyrimidin-2(1<i>H</i>)-one to Pyrimidines via PyBroP-Mediated Coupling

Abstract

An efficient two-step procedure is described to convert the Biginelli 3,4-dihydropyrimidin-2(1H)-one to various multifunctionalized pyrimidines via the Kappe dehydrogenation and a new mild PyBroP-mediated coupling with C, N, O, and S nucleophiles, which provides a readily accessible multifunctionalized pyrimidine template for diversity-oriented synthesis.