4-Amino-5-chloro-2-methoxybenzoic acid → 4-amino-5-chloro-N-[[4-(4-cyanobenzyl)-2-morpholinyl]methyl]-2-methoxybenzamide

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-aminomethyl-4-(4-cyanobenzyl)morpholine (1.5 g) in dichloromethane (40 ml), 4-amino-5-chloro-2-methoxybenzoic acid (1.2 g) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (1.3 g) are added, and the resulting mixture is stirred at 25° C. for 3 hours. The reaction mixture is washed successively with water, aqueous sodium hydroxide solution and saturated aqueous sodium chloride solution, and dried over magnesium sulfate. The solvent is distilled off under reduced pressure to give the title compound as an oil.

Provenance & Evidence