Palladium-Catalyzed Decarbonylative C-H Difluoromethylation of Azoles

钯催化唑类化合物的脱羰基CH二氟甲基化反应

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Abstract

A (XantPhos)Pd-catalyzed decarbonylative C-H functionalization of azoles with difluoromethyl anhydrides is reported. Under the optimized conditions, azole substrates react selectively at the C(2)-position to afford CF(2)H-substituted benzoxazole, oxazole, benzothiazole, thiazole, and benzimidazole products. Organometallic mechanistic studies reveal that XantPhos enforces an unusual seesaw geometry of the key Pd(II)(CF(2)H)(carboxylate) intermediate, which may be responsible for the effectiveness of this ligand.

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