N1-烷基化的3,4-二氢嘧啶-2(1H)-酮：便捷的一锅法选择性合成及其钙通道阻滞活性评估
N1-Alkylated 3,4-dihydropyrimidine-2(1H)-ones: Convenient one-pot selective synthesis and evaluation of their calcium channel blocking activity.
作者信息
Singh Kamaljit, Arora Divya, Poremsky Elizabeth, Lowery Jazmyne, Moreland Robert S
机构信息
Organic Synthesis Laboratory, Department of Applied Chemical Sciences and Technology, Guru Nanak Dev University, Amritsar 143 005, India.
出版信息
Eur J Med Chem. 2009 May;44(5):1997-2001. doi: 10.1016/j.ejmech.2008.10.002. Epub 2008 Oct 11.
It has been found that selective N1-alkylation of 3,4-dihydropyrimidine-2(1H)-ones can be achieved under solvent-less, mild phase transfer catalytic (PTC) conditions with tetrabutylammonium hydrogen sulfate and 50% aqueous NaOH as the catalyst and base, respectively. The procedure is tolerant to substitutional variation at key diversity points on the pyrimidinone moiety.
已发现，在无溶剂、温和的相转移催化（PTC）条件下，以硫酸氢四丁铵和50%的氢氧化钠水溶液分别作为催化剂和碱，可以实现3,4-二氢嘧啶-2(1H)-酮的选择性N1-烷基化。该方法对嘧啶酮部分关键多样性位点上的取代变化具有耐受性。
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