摘要
2-氨基-4-苄氧基-5-甲氧基苯甲酸甲酯是重要的有机合成中间体,在医药方面具有重要的应用价值.对其合成路线进行了优化:以香草酸甲酯为原料,经过羟基苄基化、硝化反应和选择性硝基还原合成2-氨基-4-苄氧基-5-甲氧基苯甲酸甲酯.各步反应的最佳条件(反应试剂、反应温度、反应时间、摩尔收率)分别为:羟基苄基化:丙酮,回流,3 h,93.77%;硝化:乙酸酐,0～5℃,2 h,94.40%;硝基还原:甲苯,回流,4 h,93.12%.优化后各步反应副反应少,产品纯度高,收率高,总收率达82.42%;工艺简洁,适合工业化生产.
Methyl 2-amino-4-benzyloxy-5-methoxybenzoate,which is a key pharmaceutical intermediate,has important applied value in medicament.The paper has optimized its synthesis method,which bases on hydroxyl benzylation,nitration and nitro-selective reduction.The optimal reaction conditions（solvent,temperature,time,yield） are as follows,hydroxyl benzylation,acetone,refulx,3 h,93.77%,nitration,acetic anhydride,0-5 ℃,2 h,94.40%,nitro reduction,toluene,reflux,4 h,93.12%.After the optimization,each reaction has less side reaction,the products have high purity product and overall yield of 82.42%.The process is brief and suits for industrialization.
出处
《杭州师范大学学报（自然科学版）》
CAS
2010年第4期248-251,共4页
Journal of Hangzhou Normal University(Natural Science Edition)
