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Title: Copper-Catalyzed Hydroamination of gem-Difluoroalkenes Access to Diversified α-Difluoromethyl Amines. Author: Bai D, Guo Y, Ma D, Guo X, Wu H. Journal: Org Lett; 2023 Jan 27; 25(3):533-537. PubMed ID: 36637250. Abstract: The difluoromethyl group (CF2H) is of great importance in medicinal chemistry. We report herein an efficient method for the synthesis of diversified α-difluoromethyl amines through copper-catalyzed hydroamination of gem-difluoroalkenes, where the C-N bond formed via a α-CF2H transition-metal intermediate. This new reaction proceeds through Cu-H insertion to gem-difluoroalkenes and gives valuable alkyl-CF2H-containing compounds, which overcome the much more challenged β-F elimination from α-fluoroalkyl organocopper species. The reaction exhibits broad substrate scope with readily available starting materials and commercial catalysis.[Abstract] [Full Text] [Related] [New Search]