106720-52-9Relevant academic research and scientific papers
A Cs2CO3-mediated simple and selective method for the alkylation and acylation of 3,4-dihydropyrimidin-2(1 H)-thiones
Putatunda, Salil,Chakraborty, Arijit
, p. 1057 - 1064 (2014/12/10)
Alkyl and acyl derivatives of 3,4-dihydropyrimidin-2(1H)-thiones were synthesized in good to excellent yields in the presence of Cs2CO3, a mild base. The method evidences a selective S-alkylation when using acyl chlorides as efficien
Dihydropyrimidine calcium channel blockers: 2-Heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines
Atwal,Rovnyak,Schwartz,Moreland,Hedberg,Gougoutas,Malley,Floyd
, p. 1510 - 1515 (2007/10/02)
2-Heterosubstituted-4-aryl-1,4-dihydro-6-methyl-5- pyrimidinecarboxylic acid esters 8, which lack the potential C(s) symmetry of dihydropyridine calcium channel blockers, were prepared and evaluated for biological activity. Biological assays using potassium-depolarized rabbit aorta and radioligand binding techniques showed that some of these compounds are potent mimics of dihydropyridine calcium channel blockers. The combination of a branched ester (e.g. isopropyl, sec-butyl) and an alkylthio group (e.g. SMe) was found to be optimal for biological activity. When compared directly with similarly substituted 2-heteroalkyldihydropyridines 9, dihydropyrimidines 8 were found to be 30-fold less active. The solid-state structure of dihydropyrimidine analogue 8g shows that these compounds can adopt a molecular conformation which is similar to the reported conformation of dihydropyridine calcium channel blockers.
2-substituted thio or oxy-4-aryl or heterocyclo-5-carboxy-1,4-dihydropyrimidines, composition containing them, and method of using them to reduce blood pressure
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, (2008/06/13)
1,4-Dihydropyrimidines of the formula STR1 wherein X is sulfur or oxygen and R4 is aryl or heterocyclo and disclosed. These compounds are useful as cardiovacular agents, particularly anti-hypertensive agents, due to their vasodilator activity.
