Direct Difluoromethylation of Heterocycles through Photosensitized Electron Transfer

Difluoromethylation is of prime importance for its applicability in functionalizing diverse fluorine-containing heterocycles, which are core groups in diverse biologically and pharmacologically active ingredients. Herein, we report a novel transition metal- and oxidant-free visible light-photoinduced protocol for direct C(sp(2))-H difluoromethylation of heterocycles. The reaction afforded difluoromethyl heterocycles without using colored organic dyes and metal catalysts in good yields and showed a broad substrate tolerance. Moreover, the representative products exhibited potential drug activity, and one product showed good antifungal activities against Rhizoctorzia solani (62.7 %).

Automated summary

A novel transition metal- and oxidant-free visible light-photoinduced protocol for direct C(sp(2))-H difluoromethylation of heterocycles was reported, providing difluoromethyl heterocycles in good yields with broad substrate tolerance. The representative products exhibited potential drug activity, and one product showed good antifungal activities against Rhizoctorzia solani (62.7%).