Formaldehyde → Tert-butyl 4-[(5-chloro-6-hydroxy-3-oxo-2,3-dihydrobenzofuran-7-yl)methyl]piperazine-1-carboxylate

Participants

Reaction Steps

A solution of 5-chloro-6-hydroxybenzofuran-3(2H)-one (0.185 g, 1.00 mmol) in ethanol (20 mL) was added with 1-tert-butoxycarbonylpiperazine (0.186 g, 1.00 mmol), and 37% aqueous formaldehyde (0.0812 g, 1.00 mmol) at room temperature. The mixture was stirred overnight at room temperature, and then the precipitates formed were collected by filtration, and then washed with ethyl acetate to obtain tert-butyl 4-[(5-chloro-6-hydroxy-3-oxo-2,3-dihydrobenzofuran-7-yl)methyl]piperazine-1-carboxylate (0.216 g, 56%).

Provenance & Evidence