盐酸达泊西汀的合成工艺研究  

Improved synthesis of dapoxetine hydrochloride

作　　者：尹玲丽[1] 陈国华[1] 

机构地区：[1]中国药科大学药物化学教研室,江苏南京210009

出　　处：《中国药物化学杂志》2011年第1期37-39,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的研究选择性5-羟色胺重摄取抑制剂盐酸达泊西汀的合成工艺。方法以3-苯基丙醇和1-氟萘为起始原料,经醚化、溴代、二甲胺基取代、拆分、成盐反应制得目标化合物。结果与结论目标化合物的结构经1H-NMR、MS、IR谱以及比旋光度确证。该路线原料易得,操作简便,条件温和,有利于工业化生产,消旋体收率达61.2%。For the shortcomings and deficiencies of synthesis of dapoxetine hydrochloride,the method was optimized and improved.It started from 3-phenylpropanol,which underwent etherification with 1-fluoronaphthalene in the presence of sodium hydride,followed by bromination by NBS using AIBN as catalyst,substitution with dimethyl amine,resolution by L-（＋）-tartaric acid to give dapoxetine free base and formation of dapoxetine hydrochloride with an overall yield of 21.0%.This improved process reduced the use of expensive raw materials and toxic reagents with relatively convenient operation procedure and was more suitable for large-scale industrial production.

关 键 词：选择性5-羟色胺重摄取抑制剂 盐酸达泊西汀 化学合成 工艺改进 

分 类 号：R914[医药卫生—药物化学]