2-(2,6-二氯苯胺基)苯乙酸4-(4-苯基-1,2,5-噁二唑-2-氧化物-3-)甲氧基苯甲酯的合成工艺改进  

Improved synthesis of 4-[(4-phenyl-1,2,5-oxadiazole-2-oxide-3-yl)-methoxy]benzyl 2-(2,6-dichlorophenylamino)phenylacetate

作　　者：许忻[1] 张奕华[1] 王未东[1] 

机构地区：[1]中国药科大学新药研究中心,江苏南京210009

出　　处：《中国药物化学杂志》2003年第4期222-223,229,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的改进 2 (2 ,6 二氯苯胺基 )苯乙酸 4 (4 苯基 1 ,2 ,5 二唑 2 氧化物 3 )甲氧基苯甲酯的合成工艺。方法以桂醇为原料 ,经环合、氯化、醚化及酯化 4步反应合成 2 (2 ,6 二氯苯胺基 )苯乙酸 4 (4 苯基 1 ,2 ,5 二唑 2 氧化物 3 )甲氧基苯甲酯。环合反应中 ,改用乙酸为溶剂 ;醚化反应中以乙腈代替N ,N 二甲基甲酰胺作溶剂 ;酯化反应中 ,二环己基碳化二亚胺改以滴加的方式投料。结果与结论总收率提高到 48%。本法具有反应条件温和、后处理简单、收率高等优点。Aim To improve the synthetic procedure of 4-[(4-phenyl-1,2,5-oxadiazole-2-oxide-3-yl-)-methoxyl]benzyl 2-(2,6-dichlorophenylamino)phenylacetate.Method The target compound was synthesized from cinnamic alcohol via cyclization,chlorination,etherization and esterification.In cyclization,acetic acid was used as a solvent.Acetonitrile replaced DMF as a solvent in etherisation.In esterification,DCC in dichloromethane was added dropwise to the solution.Result and Conclusion The overall yield is 48%.The improved procedure has several advantages such as mild reaction conditions,convenient operation and high yield.

关 键 词：药物化学 工艺改进 化学合成 2-(2 6-二氯苯胺基)苯乙酸4-(4-苯基-1 2 5-噁二唑-2-氧化物-3-)甲氧基苯甲酯 非甾体抗炎药 

分 类 号：TQ463[化学工程—制药化工]