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    • 1. 发明公开
    • DIFLUOROMETHYLATION REACTION OF HETEROCYCLIC RING USING TETRAFLUOROETHYLENE
    • EP4385977A1
    • 2024-06-19
    • EP22855860.7
    • 2022-08-08
    • AGC INC.
    • NOMURA, YoshitakaSUZUKI, Haruya
    • C07D215/12
    • C07D215/12
    • The aim of the present invention is to provide an easy and inexpensive method for producing difluoromethyl-substituted aromatic heterocyclic compounds in good yield. Furthermore, the aim of the present invention is to provide an easy and inexpensive method for producing aromatic heterocycle-substituted difluoroacetic acid derivatives in good yield.
      The present invention relates to a method for producing a difluoromethyl-substituted aromatic heterocyclic compound having a partial structure represented by the formula (IIa), which comprises reacting an N-oxido aromatic heterocyclic compound having a partial structure represented by the formula (Ia) with tetrafluoroethylene in the presence of a base, in a solvent selected from an aromatic hydrocarbon solvent, an ester solvent and an ether solvent.

      wherein each symbol is as described in the description.
      Furthermore, the present invention relates to a method for producing an aromatic heterocycle-substituted difluoroacetic acid derivative having a partial structure represented by the formula (IIIb), which comprises reacting an N-oxido aromatic heterocyclic compound having a partial structure represented by the formula (Ib) with tetrafluoroethylene in the presence of a compound represented by the formula (IIb): R-YH and a base, in a solvent selected from an aromatic hydrocarbon solvent, an ester solvent and an ether solvent.

      wherein each symbol is as described in the description.