6-甲氧基-7-乙氧基-4-氯喹啉的合成改进  

Improvements on the Synthesis of 6-Methoxy-7-ethoxy-4-chloroquinoline

作　　者：赵志昌[1] 王顺义[1] 闫红[1] 

机构地区：[1]北京工业大学生命科学与生物工程学院,北京100124

出　　处：《精细化工》2015年第11期1312-1315,1320,共5页Fine Chemicals

基　　金：国家科技支撑计划重点项目(2012ZX10001007-008-002)~~

摘　　要：以2-甲氧基-5-硝基苯酚为起始原料,经过O-烷基化、还原、高温合环、水解、脱羧、氯化6步反应,得到目标产物6-甲氧基-7-乙氧基-4-氯喹啉,总收率为24%。O-烷基化过程中,通过对丙酮、乙腈、DMF做溶剂的对比,发现乙腈做溶剂时,不仅产率较高,且后处理简单。在高温合环过程引入"一锅法"和"无溶剂法",不仅简化操作步骤,提高产率,而且降低了反应的污染。The synthetic methods were studied for 6-methoxy-7-ethoxy-4-chloroquinoline in details. The2-methoxy-5-nitrophenol was used as raw materials and the title compound was obtained via the Oalkylation,reduction reaction,thermal cyclization,hydrolysis,decarboxylation and chloration. The overall yield was 24%. During the O-alkylation process,compared to the acetone,acetonitrile and DMF,acetonitrile was proved to be the optimal solvent,which gave rise to the yield increased and the aftertreatment simplified. In addition,one-pot synthesis and solvent-free method were bought into the high temperature cyclization process. The one-pot method could greatly simplify the operation and improve the yield. The solvent-free reaction could reduce consumption and pollution.

关 键 词：2-甲氧基-5-硝基苯酚 6-甲氧基-7-乙氧基-4-氯喹啉 无溶剂 精细化工中间体 

分 类 号：O626.323[理学—有机化学]