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

2018 International Conference on Advanced Materials, Intelligent Manufacturing and Automation

材料科学;机械制造;运输工程

Xu, Wen Long^1 ; Guo, Cui Juan^1 ; Li, Tao^1 ; Liu, Si Quan^1

School of Chemical Engineering and Technology, University of Jinan, Jinan, Shandong

250022, China^1

关键词: Molar ratio;    Reaction conditions;    Reaction temperature;    Sulfonyl chlorides;    Total yield;   

Others  :  https://iopscience.iop.org/article/10.1088/1757-899X/382/2/022064/pdf
DOI  :  10.1088/1757-899X/382/2/022064

学科分类：材料科学（综合）

来源: IOP

【 摘 要 】

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.