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Nickel-Catalyzed Cross-Coupling of Aryl Boronic Acids with CF2Br2: Access to Diaryldifloromethanes
Xiang-Yi Chen1, Jia-Yi Shou1, Feng-Ling Qing1
1State Key Laboratory of Fluorine and Nitrogen Chemistry and Advanced Materials, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Science, Chinese Academy of Science, 345 Lingling Lu, Shanghai 200032, China.
Abstract:
Diaryldifluoromethanes are valuable structural motifs in medicinal chemistry because they can serve as bioisosteres for diaryl ether, methane, and ketone groups. However, synthetic approaches to these compounds remain limited, particularly those capable of constructing both C-C bonds of the difluoromethylene unit simultaneously. Herein, we developed a straightforward method for the synthesis of diaryldifluoromethanes via nickel-catalyzed cross-coupling of arylboronic acids with difluorodibromomethane (CF2Br2). This protocol features mild reaction conditions, exhibits broad functional group tolerance, and employs readily available starting materials.
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