N1-Alkylated 3,4-dihydropyrimidine-2(1H)-ones: Convenient one-pot selective synthesis and evaluation of their calcium channel blocking activity.
N1-Alkylated 3,4-dihydropyrimidine-2(1H)-ones: Convenient one-pot selective synthesis and evaluation of their calcium channel blocking activity.
复制标题
DOI：
10.1016/j.ejmech.2008.10.002
复制
发表时间：
2009-05
影响因子：
6.7
通讯作者：
Kamaljit Singh;D. Arora;Elizabeth Poremsky;Jazmyne Lowery;R. Moreland
中科院分区：
文献类型：
--
作者：
Kamaljit Singh;D. Arora;Elizabeth Poremsky;Jazmyne Lowery;R. Moreland
研究发现，3,4-二氢嘧啶-2(1H)- 1在无溶剂温和相转移催化（PTC）条件下，分别以四丁基硫酸氢铵和50%水溶液氢氧化钠为催化剂和碱，可实现选择性n1 -烷基化。该程序在嘧啶部分的关键多样性点上容忍取代变化。
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.