Hydrochloric Acid → N-((1-(3-(1,2,4-triazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide

Participants

Reaction Conditions

Reaction Steps

4-amino-5-chloro-2-methoxy-(piperidin-4-ylmethyl)benzamide (compound of formula 2) hydrochloride (500 mg, 1.5 mmol) was dissolved in dimethylformamide (10 mL), and 1-(3-chloropropyl)-1,2,4-triazole (compound of formula 3) (306 mg, 2.1 mmol), potassium carbonate (497 mg, 3.6 mmol), and potassium iodide (50 mg, 0.3 mmol) were added thereto. The reactants were stirred at 100° C. for 8 hours, and the reaction was terminated with the addition of water. After extraction with ethyl acetate and water, the organic layer was washed with brine, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by column chromatography to afford the title compound (55 mg, 9%).

Provenance & Evidence