第 39 卷第 4 期Vol. 39 No. 4
2009 年 8 月Aug 2009

所属栏目:医药及中间体

拉诺康唑的合成工艺研究
陈言德,孟 霆,金荣庆,张海波,李冬梅 (江苏(泰州)新药研究院,扬子江药业集团有限公司,江苏 泰州 225321)
摘 要:以1-咪唑基乙腈碳和氢氧化钾反应得到二钾盐,再与2-(1,2-二氯乙基)氯苯环合反应得到目标化合物拉诺康唑,总收率为34.0% 。关键中间体2-(1,2-二氯乙基)氯苯以邻氯苯乙烯为原料,经氯气加成得到。并研究了拉诺康唑异构体的转化。
关键词:合成;拉诺康唑;抗真菌药
中图分类号:R978.5  文献标识码:A  文章编号:1009-9212(2009)04- 0028-02
Study on Synthesis of Lanoconazole
CHEN Yan-de,MENG Ting ,JIN Rong-qing ,ZHANG Hai-bo,LI Dong-mei (Jiangsu (Taizhou) New Medicine Research Institute,Yangtze River Pharmaceutical Group,Taizhou 225321,China)
Abstract:1-Imidazolyl acetonitrile was reacted with carbon disulfide and potassium hydroxide to give a dipotassium salt. The later was further converted to lanoconazole by reaction with 2-(1,2- dichloro-ethyl)chlorophenyl,which was prepared from o-chlorostyrene. The overal yield of the process was 34.0%. Conversion of the isomers of lanoconazole was also studied.
Key words:synthesis;lanoconazole;antifungal agent
作者简介:陈言德(1984-),男,江苏泗洪人,助理工程师,主要从事有机合成及原料药的开发工作。(E-mail:chenyande86@163.com)
收稿日期:2009-06-08