Hydrochloric Acid → HCID 131722847, compound

Participants

Reaction Steps

Methanesulfonyl chloride (0.071 ml, 0.92 mmol) and 4-dimethylaminopyridine (catalytic amount) were added to a solution of 2-[(2R)-(3,4-dichlorophenyl)-4-(cyclobutanecarbonyl)morpholin-2-yl]ethanol (219 mg, 0.61 mmol), which was prepared in Example 1(a), in pyridine (2 ml) with ice-cooling under a nitrogen atmosphere. The mixture was stirred at the same temperature for 30 minutes. The reaction mixture was acidified with ice-cooled hydrochloric acid (10%) and extracted with ethyl acetate. The organic layer was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous magnesium sulfate. The ethyl acetate was distilled off under reduced pressure. The residue was purified by silica gel thin layer chromatography using n-hexane/ethyl acetate=¼ as a developing solvent to afford the desired compound (255 mg, 96%) as a white amorphous solid.

Provenance & Evidence