第 39 卷第 4 期 | | Vol. 39 No. 4 | 2009 年 8 月 | Aug 2009 |
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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 |
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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 |
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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)
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收稿日期:2009-06-08
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