Department of Chemistry, Maulana Azad College, 8 Rafi Ahmed Kidwai Road, Kolkata 13, India.
Eur J Med Chem. 2012 Aug;54:223-31. doi: 10.1016/j.ejmech.2012.04.043. Epub 2012 May 16.
A regioselective N1-alkylation of 3,4-dihydropyrimidin-2(1H)-ones using a very efficient mild base Cs(2)CO(3) and alkyl halides at room temperature has been reported. The selectivity of this methodology is excellent and the yields of the alkylated products are very good. Furthermore inhibitory action of both the 3,4-dihydropyrimidin-2(1H)-ones and the N1-alkylated derivatives were tested on Ca(2+)-ATPase, which revealed that the parent compounds can act as Ca(2+)-ATPase inhibitors whereas the N1-alkylated derivatives are inefficient for this purpose.
已报道一种使用高效温和碱 Cs(2)CO(3)和卤代烷烃在室温下对 3,4-二氢嘧啶-2(1H)-酮进行区域选择性 N1-烷基化的方法。该方法的选择性非常好，烷基化产物的收率也非常高。此外，还测试了 3,4-二氢嘧啶-2(1H)-酮及其 N1-烷基衍生物对 Ca(2+)-ATP 酶的抑制作用，结果表明，母体化合物可以作为 Ca(2+)-ATP 酶抑制剂，而 N1-烷基衍生物则对此没有作用。
