Abstract
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.
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Acknowledgements
This work was supported by the DICP and K. C. Wong Education Foundation (GJTD-2020-08).
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Difluoroalkylative Carbonylation of Alkenes to Access Carbonyl Difluoro-containing Heterocycles: Convenient Synthesis of GeMigliptin
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Bao, ZP., Zhang, Y., Wang, LC. et al. Difluoroalkylative carbonylation of alkenes to access carbonyl difluoro-containing heterocycles: convenient synthesis of gemigliptin. Sci. China Chem. 66, 139–146 (2023). https://doi.org/10.1007/s11426-022-1439-1
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DOI: https://doi.org/10.1007/s11426-022-1439-1