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Difluoroalkylative carbonylation of alkenes to access carbonyl difluoro-containing heterocycles: convenient synthesis of gemigliptin
2022, Bao, Zhi-Peng, Zhang, Youcan, Wang, Le-Cheng, Wu, Xiao-Feng
Fluorinated heterocycles play a vital role in pharmaceutical and agrochemical industries. Hence, rapid and efficient construction of fluorinated heterocycles remains highly demanded. Herein, a difluoroalkylative carbonylative cyclization of unactivated alkenes and ethylene gas enabled by palladium catalysis has been developed for the first time toward the synthesis of α-carbonyl difluoro-modified glutarimides. This procedure can also be applied to the synthesis of GeMigliptin which is a medicine approved for the treatment of type 2 diabetes mellitus. [Figure not available: see fulltext.]