Formic Acid → 4-(4-Bromo-7-methoxybenzofuran-2-ylmethoxy)-1-methyl-piperidine

Participants

Reaction Conditions

Reaction Steps

4-(4-Bromo-7-methoxybenzofuran-2-ylmethoxy)-piperidine (0.98 g), formic acid (0.65 ml) and formaldehyde (0.56 g of a 37% w/w solution in water) were combined and heated to 95° C. overnight. After cooling to room temperature the mixture was diluted with water (70 ml) and a concentrated aqueous solution of sodium hydroxide added until the solution was basic (pH=14). It was extracted with ethyl acetate (2×100 ml). The combined organic extracts were dried over magnesium sulfate and concentrated in vacuo to afford the title compound as a pale yellow oil (1.03 g).

Provenance & Evidence