Difunctionalization of gem-difluoroalkenes for amination and heteroarylation via metal-free photocatalysis

Subjects: Pharmaceutical Science >> Medicinal Chemistry submitted time 2024-09-20

Zhong, Yuanchen Zhuang, Zhen Zhang, Xiaofei Xu, Bin Yang, Chunhao

Abstract： gem-Difluoroalkenes are widely used building blocks in fluorine chemistry. Herein, a metal-free photocatalytic amination and heteroarylation method of gem-difluoroalkenes with heteroaryl carboxylic acid oxime esters as substrates is reported. This environmentally benign reaction proceeds via radical-radical cross-coupling in energy-transfer-mediated photocatalysis and can be used in the rapid construction of heteroaryl difluoroethylamine scaffolds and late-stage modification of complex pharmaceutical structures.

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