Process Optimization of Methyl 2-Methoxy-5-Aminosulfonyl Benzoate

Methyl 2-methoxy-5-aminosulfonyl benzoate as an intermediate of sulpiride was synthesized from salicylic acid as precursor, which generally consisted of four reactive steps as to etherification, sulfonyl chloride, amine and lipid. Here in, after optimization of reaction conditions such as molar ratio, reaction time and reaction temperature, the yield of the four-step reactions can be improved as to 92.6% (etherification), 95.7% (sulfonyl chloride), 75.8% (amine) and 97.4%(esterification), respectively, which resulted to the efficient improvement of total yield (63.7%). The structures and purity of all synthesized compounds was confirmed by ¹HNMR and HPLC. (paper)