毒扁豆碱的合成前体化合物的制备研究

Preparation Study of Synthetic Precursor Compounds of Physostigmine

本文以5-甲氧基色胺为起始原料,经胺基保护、分子内环化、甲基化及酰胺还原四步反应制备毒扁豆碱(Physostigmine)合成前体。该合成路线具有合成试剂价廉易得、合成操作简便、对环境友好等优点,工业化生产可行性高。作为毒扁豆碱(Physostigmine)的合成前体,本中间体也同样可作为苯胺基甲酸酯毒扁豆酚碱(Phenserine)以及各类毒扁豆碱衍生物的合成前体,因此具有很好的应用价值和发展潜力。

This paper took 5-methoxytryptamine as the starting material to prepare synthetic precursors of physostigmine through four step reaction:amino protection,intramolecular cyclization,methylation and amide reduction.The advantages of the synthetic route were simple,inexpensive synthesis reagents,simple synthetic operation and friendly to the environment.The feasibility of industrial production was high.As synthetic precursor compounds of physostigmine,the intermediates could also be used for precursors of aniline formate eseroline(phenserine)and various physostigmine derivatives,so it had good application value and development potential.