31408-36-3Relevant academic research and scientific papers
Preparation of 2,5-disubstituted pyrimidines from vinamidinium salts and synthesis of novel disulfane derivatives
Rafiee Samani, Ziba,Mehranpour, Abdolmohammad,Hasaninejad, Alireza
supporting information, p. 2150 - 2156 (2020/03/10)
Novel pyrimidine derivatives were prepared from the reaction of 2-substituted 1,3-bis(dimethylamino)-trimethinium salts with thiourea or guanidine in the presence of ethyl-diisopropylamine in ethanol at reflux, and also some 5-substituted pyrimidine-2-thi
Regioselective synthesis of novel 4,5-diaryl functionalized 3,4-dihydropyrimidine-2(1H)-thiones via a non-Biginelli-type approach and evaluation of their in vitro anticancer activity
Sosnicki, Jacek G.,Struk, Lukasz,Kurzawski, Mateusz,Peruzynska, Magdalena,Maciejewska, Gabriela,Drozdzik, Marek
supporting information, p. 3427 - 3440 (2014/05/20)
An easy and novel approach to synthesize 4,5-diaryl functionalized 3,4-dihydropyrimidine-2(1H)-thiones via addition of aryllithiums to 5-aryl substituted pyrimidine-2(1H)-thiones, which could be regarded as a method complementary to the most widely used Biginelli-type synthesis, is described. In the reaction of aryllithiums with N-(Me)Bn substituted pyrimidine-2(1H)-thiones a high degree of regioselectivity of addition, leading to 4-aryl adducts, was achieved. Selected compounds tested for their in vitro anticancer activity against four human cancer cell lines showed the greatest activity against breast cancer (MCF7). 1-Benzyl-4-(3-hydroxyphenyl)-5-phenyl substituted 3,4-dihydropyrimidine-2(1H)-thione (10g) exhibiting 10-fold more potent activity than the best known monastrol (MON) stands as a promising candidate for further scaffold and asymmetric synthesis. the Partner Organisations 2014.
