盐酸达泊西汀的合成工艺改进  

Improved synthesis of dapoxetine hydrochloride

作　　者：孙铭[1,2] 白洁 张作鹏 刘洋 SUN Ming;BAI Jie;ZHANG Zuo-peng;LIU Yang(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China;Northeast Pharmaceutical Group Co.,Ltd.,Shenyang 110027,China)

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]东北制药集团股份有限公司,辽宁沈阳110027

出　　处：《中国药物化学杂志》2019年第2期122-125,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的对达泊西汀的合成工艺进行改进。方法以3-氯-1-苯丙酮为起始原料,经过还原、取代、酯化、胺化、拆分、成盐反应,得到盐酸达泊西汀。结果与结论目标化合物的结构经质谱、氢谱和碳谱确证。总收率纯度为29.3%,纯度为99.7%。该方法具有经济可行、操作简便等优点,适合工业化生产。Dapoxetine is an oral medication for the treatment of premature ejaculation.Based on the literatures and patents,a new synthetic route to dapoxetine was established,and the synthetic process was also investigated and optimized thoroughly.With 3-chloropropiophenone as the starting material,dapoxetine was synthesized via reduction,substitution,esterification,amination,resolution and salt formation.The total yield was 29.3%and the purity of the final product was 99.7%(HPLC).The structure of dapoxetine was confirmed by ESI-MS,1H-NMR and 13C-NMR.The improved process has the advantages of low cost and high purity,and is suitable for industry.

关 键 词：3-氯-1-苯丙酮 达泊西汀 工艺改进 

分 类 号：R914[医药卫生—药物化学]