Formaldehyde → 3-Chloro-4-(1-methylpiperidin-4-yloxy)nitrobenzene

Participants

Reaction Conditions

Reaction Steps

To a suspension of 4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-chloronitrobenzene (1.50 g) obtained in reference example 3 in 90% formic acid (4.00 g) was added 37% formaldehyde (2.50 g), and the resulting mixture was stirred at 100° C. for 2 hours. After cooling to room temperature, the reaction mixture was neutralized with an aqueous potassium carbonate 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 to afford the title compound (1.12 g, yield: 98%) as a yellow solid.

Provenance & Evidence