4-羟基吲哚和4-甲氧基吲哚的合成  

Synthesis of 4-hydroxyindole and 4-methoxyindole

作　　者：吴秋业[1] 潘涛 金永生[1] 潘亚菊[1] 俞世冲[1] 廖洪利[1] 

机构地区：[1]第二军医大学药学院,上海200433 [2]国际妇幼保健院,上海200004

出　　处：《中国药物化学杂志》2003年第1期25-27,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的寻找操作方便、反应路线短且成本低的工艺路线。方法通过取代酚的醚化 ,再在苯环上直接引入腈乙基 ,然后水解、环合等反应 ,直接生成吲哚衍生物。结果采用氢的亲核取代反应(VNS) ,直接制得 4 羟基吲哚和 4 甲氧基吲哚 ,操作方便 ,反应路线短且成本较低。结论 4 羟基吲哚和 4 甲氧基吲哚的收率分别达 5 7 4%和 2 8 8% ,是值得研究推广的新工艺。Aim To look for a new method of synthesizing 4-hydroxyindole and 4-methoxyindole.Methods and Results Through the reaction of alkylation of substituted phenols,hydrolysis and cyclization,“vicarious nucleophilic substitution of hydrogen(VNS)” was used to synthesize 4-hydroxyindole and 4-methoxyindole,the method is simple and the cost is low.Conclusion The overall yields of 4-hydroxyindole and 4-methoxyindole are 57.4% and 28.8%,respectively.The process is cheaper and simpler.

关 键 词：4-羟基吲哚 4-甲氧基吲哚 合成 药物化学 制备 氢的亲核取代反应 

分 类 号：R914[医药卫生—药物化学]