美乐托宁的合成新工艺研究  

Study on the new synthetic method for melatonin

作　　者：万宁[1] 巨佳[1] 张芳芳[1] 邱海[1] 赵卓[1] 周四元[1] 张邦乐[1] 

机构地区：[1]第四军医大学药学院药剂学教研室,西安710032

出　　处：《西北药学杂志》2013年第3期304-306,共3页Northwest Pharmaceutical Journal

基　　金：国家"重大新药创制"科技重大专项基金(No.2011ZXJ09106-04C);校精英人才"青年英才支持计划"研究基金资助项目(编号:20110701)

摘　　要：目的建立一种新的反应条件温和、步骤简短的美乐托宁合成路线。方法以4-甲氧基苯肼盐酸盐和2,3-二氢呋喃为原料,经缩合环化、氨化和乙酰化三步制得美乐托宁,所得中间体和目标产物的化学结构经熔点、1 H-NMR和质谱进行鉴定。结果合成中间体和产物的化学结构与目标化合物结构一致。结论该合成路线条件温和,原料易得,工艺简短,三步总收率达54.6%。Objective To establish a novel synthetic route of melatonin with milder reaction conditions, shorter steps, and higher total yield. Method Starting with 2,3-dihydrofuran and 4-methoxyphenylhydrazine hydrochloride, 3-aminoethyl-5-methoxy-lH-indole was obtained through cyclocondensation and ammonification. Melatonin was prepared via acetylation of 3-aminoethyl-5-methoxy- 1 H-indole. The chemical structure of the target products was confirmed by 1 H-NMR, MS and melting point. Results The structure of the obtained compounds was in accordance with the literature. Conclusion This method has some advantages,such as readily a- vailable raw materials,milder conditions and shorter steps. The total yield （up to 54.6 %） was higher than that of literatures.

关 键 词：美乐托宁 化学合成 合成工艺 

分 类 号：R914.5[医药卫生—药物化学]