非甾体抗炎药洛索洛芬钠的合成  

Synthesis of Nonsteroidal Anti-inflammatory Drug Loxoprofen Sodium

作　　者：吴朝刚 周雄飞 庄程翰 沈杭州 张兴贤[2] 

机构地区：[1]浙江普洛家园药业有限公司,浙江东阳322118 [2]浙江工业大学药学院,浙江杭州310032

出　　处：《合成化学》2017年第4期356-359,共4页Chinese Journal of Synthetic Chemistry

摘　　要：以1-苯基-2-氯-1-酮为原料,经缩酮保护、重排、水解、酯化及氯甲基化等反应制得关键中间体2-(4-氯甲基苯基)丙酸甲酯(7);7与2-乙氧羰基环戊酮缩合后,再经脱羧及成盐反应合成了洛索洛芬钠,总收率36%,其结构经~1H NMR和MS(ESI)确证。The key intermediate, methyl 2-（4-chloromethylphenyl ） propionate （7）, was prepared by five steps of ketalization, rearrangement, hydrolysis, esterifieation and ehloromethylation, using 1-phe- nyl-2-ehloro-l-one as starting material. Loxoprofen sodium with overall yield of 36% was synthesized from 7 by phase-transfer eatalyzed alkylation with ethyl 2-oxoeyclopentaneearboxylate, and then decar- boxylation and salt formation. The structure was confirmed by 1H NMR and MS（ESI）.

关 键 词：1-苯基-2-氯-1-酮 氯甲基化反应 非甾体抗炎药 洛索洛芬钠 药物合成 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]