Trimethylsilyl cyanide → N-(2-cyanocyclohexyl)-3,5-difluoro-4-(2-propynyloxy)benzamide

関与物質

反応条件

反応手順

At room temperature, 99 mg of trimethylsilyl cyanide was added dropwise to a mixture of 12 ml of tetrahydrofuran and 291 mg of 7-[3,5-difluoro-4-(2-propynyloxy)benzoyl]-7-azabicyclo[4.1.0]heptane and, further, tetrabutylammonium fluoride (0.05 ml of 1M tetrahydrofuran solution) was added. The resulting mixture was heated with stirring at 40° C. for 8 hours. The reaction mixture was concentrated under reduced pressure. The residue was subjected to silica gel column chromatography to obtain 0.24 g of N-(2-cyanocyclohexyl)-3,5-difluoro-4-(2-propynyloxy)benzamide (hereinafter, described as the compound 80 of the present invention) represented by the formula:

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