阿巴卡韦中间体2-杂氮双环[2,2,1]庚-5-烯-3-酮的合成  

Synthesis of 2-Azabicyclohept-5-en-3-one as an Intermediate for Abacavir

作　　者：陈灿[1] 郭莉娜[2] 李宏伟[2] 侯仲轲[1] 

机构地区：[1]湖南化工研究院药物研究所,湖南长沙410007 [2]华中师范大学,湖北武汉430079

出　　处：《精细化工中间体》2006年第5期36-38,共3页Fine Chemical Intermediates

摘　　要：采用一步法由对甲基苯亚磺酸钠与氯化氰及1,3-环戊二烯合成目标物2-杂氮双环[2,2,1]庚-5-烯-3-酮。反应条件为:n(对甲基苯亚磺酸钠)∶n(氯化氰)∶n(1,3-环戊二烯)=0.48∶1.05∶1,反应温度控制在15℃,反应7h,反应中控制pH=5,可得纯度为95%的产品,收率由文献报道的64%提高到78%。2-Azabicyclo [2,2,1]hept-5-en-3-one was synthesized from sodium-p-toluene sulfinate with cyanogens chloride and cyclopentadiene by one-pot process. The optimal conditions were as follow： the mole ratio of sodium-p-toluene sulfinate：cyanogens chloride：cyclopentadiene was 0.48：1.05：1, the reaction temperature 15℃, reaction time 5 h and pH of the reaction 5. Under these optimal conditions, the purity of product was 95%, and The yield was increased from 64% to 78%.

关 键 词：一步法 合成 2-杂氮双环[2 2 1]庚-5-烯-3-酮 

分 类 号：TQ463[化学工程—制药化工]