Formaldehyde → HCID 22181168, compound

Participants

Reaction Conditions

Reaction Steps

To a suspension of 4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-trifluoromethylnitrobenzene (2.45 g) obtained in reference example 100 in 90% formic acid (8.80 g) was added 37% formaldehyde (5.50 g), and the resulting mixture was stirred at 100° C. for 6 hours. After cooling to room temperature, the reaction mixture was neutralized with an aqueous sodium hydrogencarbonate solution and extracted with ethyl acetate. The extract was washed with a saturated aqueous sodium chloride solution, dried over anhydrous magnesium sulfate and evaporated in vacuo. The residue obtained was purified by chromatography on a silica gel column using a mixed solvent of dichloromethane and methanol (10:1) as the eluent to afford the title compound (1.82 g, yield: 95%) as a yellow oil.

Provenance & Evidence