反应详情

The 5-azidomethyl-2-[(4-chlorophenylsulfonyl)(2,5-difluorophenyl)methyl]pyridine (230 mg, 0.529 mmol) obtained in Example 350 and palladium on carbon (46 mg) were added to a mixture of ethyl acetate (15 ml) and ethanol (15 ml). The resulting mixture was stirred for 45 minutes under 1 atom hydrogen atmosphere. After filtration, the filtrate was concentrated under reduced pressure. The residue thus obtained was dissolved in dichloromethane (5 ml). Triethylamine (70 μl, 0.499 mmol) and di-tert-butyl carbonate (174 mg, 0.996 mmol) were added to the resulting solution. The mixture was stirred at room temperature for 3 days. The reaction mixture was concentrated under reduced pressure. The residue thus obtained was subjected to flash chromatography on a silica gel column. A fraction obtained from the elution portion with hexane:ethyl acetate=4:1 was concentrated under reduced pressure, whereby title compound (78 mg, 0.153 mmol, 37%) was obtained as a colorless amorphous substance.

1. filtrationAfter filtration
2. concentrationthe filtrate was concentrated under reduced pressure
3. customThe residue thus obtained
4. concentrationThe reaction mixture was concentrated under reduced pressure
5. customThe residue thus obtained
6. concentrationethyl acetate=4:1 was concentrated under reduced pressure