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.
An efficient two-step procedure is described to convert the Biginelli 3,4-dihydropyrimidin-2(1H)-one to various multifunctionalized n class="Chemical">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.
Authors: Shyh-Ming Yang; Daniel J Urban; Makoto Yoshioka; Jeffrey W Strovel; Steven Fletcher; Amy Q Wang; Xin Xu; Pranav Shah; Xin Hu; Matthew D Hall; Ajit Jadhav; David J Maloney Journal: Bioorg Med Chem Lett Date: 2018-08-31 Impact factor: 2.823