77186-59-5Relevant academic research and scientific papers
Preparation of 3,4-Substituted-5-Aminopyrazoles and 4-Substituted-2-Aminothiazoles
Havel, Stepan,Khirsariya, Prashant,Akavaram, Naresh,Paruch, Kamil,Carbain, Benoit
, p. 15380 - 15405 (2019/01/04)
3,4-Substituted-5-aminopyrazoles and 4-substituted-2-aminothiazoles are frequently used intermediates in medicinal chemistry and drug discovery projects. We report an expedient flexible synthesis of 3,4-substituted-5-aminopyrazoles (35 examples), based on palladium-mediated α-arylation of β-ketonitriles with aryl bromides. A library of 4-substituted-2-aminothiazoles (21 examples) was assembled by a sequence employing Suzuki coupling of newly prepared, properly protected pinacol ester and MIDA ester of 4-boronic acid-2-aminothiazole with (hetero)aryl halides.
Potential antimalarials. XXII Some 2,4-diamino-5-(3- and 4-trifluoromethylphenyl and 3,4-methylenedioxyphenyl)pyrimidines
Barlin, Gordon B.,Kotecka, Barbara,Rieckmann, Karl H.
, p. 647 - 650 (2007/10/03)
A series of 10 pyrimethamine analogues containing 3′- and 4′-trifluoromethyl and 3′,4′-methylenedioxy groups has been prepared and tested for in vitro antimalarial activity against the FC-27 and K-1 isolates of Plasmodium falciparum. Several of these compounds were almost as active as pyrimethamine against the drug-sensitive FC-27 isolate, and like pyrimethamine, they were much less active against the drug-resistant K-1 isolate. The 4′-trifluoromethyl compunds, however, showed much smaller differences.
