Preparation of 3,4-Substituted-5-Aminopyrazoles and 4 Substituted-2-Aminothiazoles

Varování

Publikace nespadá pod Filozofickou fakultu, ale pod Přírodovědeckou fakultu. Oficiální stránka publikace je na webu muni.cz.

Autoři	HAVEL Štěpán KHIRSARIYA PrashantKumar AKAVARAM Naresh PARUCH Kamil CARBAIN Benoit Jean-Pierre
Rok publikování	2018
Druh	Článek v odborném periodiku
Časopis / Zdroj	The Journal of Organic Chemistry
Fakulta / Pracoviště MU	Přírodovědecká fakulta
Citace
www	http://dx.doi.org/10.1021/acs.joc.8b02655
Doi	http://dx.doi.org/10.1021/acs.joc.8b02655
Klíčová slova	synthesis; medicinal chemistry; building blocks; aminopyrazole; aminothiazole
Popis	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 alfa-arylation of beta-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.
Související projekty:	Novel efficient and selective inhibitors of MRE11 nuclease and their potential therapeutic implications CZ-OPENSCREEN: National Infrastructure for Chemical Biology