Publication details

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


HAVEL Štěpán KHIRSARIYA PrashantKumar AKAVARAM Naresh PARUCH Kamil CARBAIN Benoit Jean-Pierre

Year of publication 2018
Type Article in Periodical
Magazine / Source The Journal of Organic Chemistry
MU Faculty or unit

Faculty of Science

Keywords synthesis; medicinal chemistry; building blocks; aminopyrazole; aminothiazole
Description 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.
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