Abstract
A simple transition-metal-free and highly chemoselective strategy for the preparation of C-3 arylated 1H-pyrazoles with enaminones and p-toluenesulfonyl hydrazide (TsNHNH2) has been developed. The current environmental benign protocols showed that, TsNHNH2 could be served as the safe and easy-to-handle hydrazide for the preparation of C-3 arylated 1H-pyrazoles instead of the explosive and genotoxic hydrazine hydrate under mild conditions, with broad substrate scope and excellent functional group tolerance. More importantly, a gram-scale synthesis of a synthetic equivalent of key intermediate to immuno-oncology agonist BMS-986299 was demonstrated successfully through a simple crystallization or extraction process for the scalable production.
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