Efficient conversion of Biginelli 3,4-dihydropyrimidin-2(1H)-one to pyrimidines via PyBroP-mediated coupling |
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| Authors: | Kang Fu-An Kodah Jason Guan Qunying Li Xiaobing Murray William V |
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| Institution: | Johnson & Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Raritan, New Jersey 08869, USA. fkang@prdus.jnj.com |
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| 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. |
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