摘要
[目的]探讨3,4-二甲氧基苄胺的合成方法。[方法]设计两条合成路线:路线Ⅰ,以香兰素为原料,经甲基化、肟化及铝镍合金还原得目标物;路线Ⅱ,以3,4-二甲氧基苯甲酸为原料,经氯化、氨解及还原得目标物。[结果]两种方法所合成的目标物结构经ESI(+)Ms、1HNMR得以确证;路线Ⅰ总收率为81.7％,路线Ⅱ总收率为55.6％。[结论]路线Ⅰ收率高,操作简便,较适于产业化。
[AIM] To investigate the synthesis of 3,4-dimethoxybenzylamine. [METHODS] Two routes for the synthesis of the target compound were devised. Route Ⅰ : Vanillin was chosen as the starting material to prepare the target compound via methylation, oxidation and reduction with Raney Nickel (Al/Ni Alloy); Route Ⅱ : 3, 4-Dimethoxybenzoic acid was chosen as the starting material to prepare the target compoud via chlorization, amidation and reduction with borohydride potassium. [RESULTS] The target compound was synthesized by the above routes, and its structure was confirmed by MS and 1HNMR. [CONCLUSION] Route Ⅰ , by which the target compound was obtained with 81. 7% overall yield, is suitable for industrial manufacture.
出处
《药学进展》
CAS
2003年第4期225-227,共3页
Progress in Pharmaceutical Sciences
