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Download filePreparation of 3,4-Substituted-5-Aminopyrazoles and 4‑Substituted-2-Aminothiazoles
dataset
posted on 2018-11-21, 00:00 authored by Stepan Havel, Prashant Khirsariya, Naresh Akavaram, Kamil Paruch, Benoit Carbain3,4-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.