5-(3,4-二氯苯基)-二氢-2-呋喃酮合成方法的改进  

A New Method of Preparing 5-(3,4-Dichloro-phenyl)-dihydro-furan-2-one

作　　者：滕雅娣[1] 王思林[1] 曲晓晔[1] 

机构地区：[1]沈阳化工学院应用化学学院,辽宁沈阳110142

出　　处：《化学世界》2006年第4期232-234,共3页Chemical World

摘　　要：采用4-(3,4-二氯苯基)-4-氧代丁酸为原料,研究了抗抑郁药物盐酸舍曲林的中间体5-(3,4-二氯苯基)-二氢-2-呋喃酮的合成方法。实验发现有效消除泡沫和杂质以及缩短反应周期的方法:硼氢化钠加完后补加1 mL氢氧化钠溶液、中途过滤、晶体形成时期用冰水浴,使所得产品较纯净而且将关环反应时间由文献的16 h降低为4 h,产品收率达到94%。5-（3,4-Dichloro-phenyl）-dihydro-furan-2-one, an important intermediate of Sertraline hydrochloride which is a more effective drug for treatment of antidepressant, was prepared from 4- （3,4-dichloro-phenyl）-4-oxygenic-butyric-acid. A method to remove bubbles to get rid of impurity and to decrease the time of the reaction was found, i.e. to add 1 mL aqueous sodium hydroxide after adding sodium borohydride, to filtrate, intermediately to crystallize in an ice water bath. The reaction time was decreased from 16h to 4h, and the yield was 94%.

关 键 词：盐酸舍曲林 硼氢化钠 中间体 

分 类 号：O626.11[理学—有机化学]