Efficient conversion of Biginelli 3,4-dihydropyrimidin-2(1H)-one to pyrimidines via PyBroP-mediated coupling.
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.
Kang
Fu-An
FA
Johnson & Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Raritan, New Jersey 08869, USA. fkang@prdus.jnj.com
Kodah
Jason
J
Guan
Qunying
Q
Li
Xiaobing
X
Murray
William V
WV
D006865:Hydrogenation; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis*; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry*
D011743:Pyrimidines; D011744:Pyrimidinones