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

Varování

Publikace nespadá pod Fakultu sportovních studií, 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