反应详情

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 0.2 ml (1.8 mmol) of n-propyl 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. The crude product obtained after purification by chromatography (silica gel; toluene/ethanol/ethyl acetate 8/1/1) was crystallized from ethyl acetate. 155 mg (33%) of the title compound were obtained as a colorless solid.

1. additionThe reaction mixture was poured onto ice/2 M hydrochloric acid
2. filtrationthe precipitated solid was filtered off with suction
3. washwashed with water until neutral
4. customThe crude product obtained
5. customafter purification by chromatography (silica gel; toluene/ethanol/ethyl acetate 8/1/1)
6. customwas crystallized from ethyl acetate