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Abstract
A practical synthesis of pyrazol-4-thiols from a diverse 4-iodopyrazoles has been developed. The elaborated procedure is based on Cu-catalyzed C-I to C-S exchange using PhC(O)SH as “SH-surrogate” with subsequent mild benzoyl cleavage without intermediate S-(R-1H-pyrazol-4-yl) benzoylthiolates purification. The approach is tolerant to reactive functional groups, such as nitrile, esters, and Boc-protected amine moiety in the pyrazole core. Easy scale-up protocols to the 10-50g scale, avoiding chromatographic purification, were described.
