Cesium carbonate → 5-Chloro-2-methoxy-N-(2-(1-(3-methylthioureidosulfonyl)piperidin-4-yl)ethyl)benzamide

Participants

Reaction Steps

376 mg (1 mmol) of 4-(2-(5-chloro-2-methoxybenzamido)ethyl)piperidine-1-sulfonamide and 652 mg (2 mmol) of cesium carbonate were heated in 5 ml of N-methyl-2-pyrrolidone with 73 mg (1 mmol) of methyl isothiocyanate at 80° C. for 10 minutes. The reaction mixture was poured onto ice/2 M hydrochloric acid, and the precipitated solid was filtered off with suction and washed with water until neutral. Purification by chromatography (silica gel; toluene/ethanol/ethyl acetate 8/1/1) resulted in 90 mg (20%) of the title compound as a colorless solid.

Provenance & Evidence