Hydrochloric Acid → Da-6886

Participants

Reaction Conditions

Reaction Steps

4-amino-5-chloro-2-methoxy-(piperidin-4-ylmethyl)benzamide (compound of formula 2) hydrochloride (400 mg, 1.2 mmol) was dissolved in dimethylformamide (10 mL), and 3-(1,2,3-triazol-1-yl)propyl methanesulfonate (compound of formula 3) (344 mg, 1.68 mmol), triethylamine (0.5 mL, 3.591 mmol), potassium carbonate (232 mg, 1.68 mmol), and potassium iodide (40 mg, 0.24 mmol) were added thereto, followed by stirring at 120° C. for 4 hours. After the reaction was completed, the reactants were cooled to room temperature, extracted with ethyl acetate and water, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The resulting residue was purified by column chromatography to afford the title compound (185 mg, 38%).

Provenance & Evidence