第 45 卷第 1 期Vol. 45 No. 1
2015 年 2 月Feb 2015

所属栏目:医药及中间体

2-苯并噻唑磺酰氯的合成
方武宏,侯 霄,刘学龙,陈国良* (沈阳药科大学 基于靶点的药物设计与研究教育部重点实验室, 辽宁 沈阳 110016)
摘 要:以2-巯基苯并噻唑和10%次氯酸钠溶液为原料合成2-苯并噻唑磺酰氯。优化反应条件:当n(2-巯基苯并噻唑)∶n(次氯酸钠)=1.00∶6.12,反应温度为-10℃,反应时间6 h,优化条件下产物收率达85.8%,其结构经ESI-MS和1H NMR确证。
关键词:2-苯并噻唑磺酰氯;2-巯基苯并噻唑;合成
中图分类号:TQ463  文献标识码:A  文章编号:1009-9212(2015)01-0061-02
Synthesis of Benzothiazole-2-sulfonyl Chloride
FANG Wu-hong, HOU Xiao, LIU Xue-long, CHEN Guo-liang* (Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China)
Abstract:Benzothiazole-2-sulfonyl chloride was prepared using 2-mercaptobenzothiazole and 10% sodium hypochlorite as raw materials. When the molar ratio of 2-mercaptobenzothiazole to10% sodium hypochlorite was 1∶6.12; the reaction temperature was -10℃; and the reaction time was 6 h; the yield of Benzothiazole-2-sulfonyl chloride was 85. 8%. Chemical structure of the final product was also confirmed using 1H NMR and ESI-MS.
Key words:benzothiazole-2-sulfonyl chloride; 2-mercaptobenzothiazole; synthesis
作者简介:方武宏(1990-),男,广东汕头人,硕士研究生,主要从事药物合成和工艺研究(E-mail:519776261@qq.com)。
联 系 人:陈国良,教授,博士生导师,主要从事抗癌药物的研究(E-mail:guuliang222@gmal.com)。
收稿日期: 2014-12-0