4,6-二氯吲哚的合成研究  

Study on the synthesis of 4,6-dichloro-1H-indole

作　　者：徐桂清 王家豪 毛龙飞 李伟 XU Gui-qing;WANG Jia-hao;MAO Long-fei;LI Wei(School of Chemistry and Chemical Engineering,Henan Engineering Research Center of Chiral Hydroxyl Pharmaceutical,Henan normal university,Xinxiang 453007,China)

机构地区：[1]河南师范大学化学化工学院,河南省手性醇类药物工程技术研究中心,河南新乡453007

出　　处：《化学研究与应用》2018年第12期2017-2020,共4页Chemical Research and Application

基　　金：2015年河南重点科技攻关项目(152102210285)资助.

摘　　要：本文以3,5-二氯苯胺为原料,先与亚硝酸钠和2-甲基乙酰乙酸乙酯经一锅法发生重氮化和胺醛缩合反应得到芳腙类化合物,然后芳腙类化合物在多聚磷酸作用下发生费歇尔吲哚环合反应得到4,6-二氯吲哚甲酸乙酯,最后经过酯水解后和含铜化合物催化脱羧得到4,6-二氯吲哚,总收率达到50%,该方法操作简单,反应条件温和,适合工业化生产。4,6-dichloro-1 H-indole is a key intermediate in the synthesis of new drugs.3,5-Dichloroaniline was used as the starting material to obtain the target compound via multi-step reactions,including diazotization,condensation reaction,Fischer indole synthesis,hydrolysis reaction and decarboxylation.After the reaction conditions were optimized,the total yield of this route reached 50%. The advantages of this route included easy-to-access raw materials,high yield,simple operation,and it was suitable for industrialscale production.

关 键 词：3 5-二氯苯胺 重氮化 胺醛缩合 费歇尔吲哚环合 4 6-二氯吲哚 

分 类 号：O623.6[理学—有机化学]