| 8-氯-10,11-二氢-4-氮杂-5H-二苯并[a,d]-5-环庚酮的合成新方法 |
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| 引用本文： | 谢艳,吾国强,郑土才,陈芬儿. 8-氯-10,11-二氢-4-氮杂-5H-二苯并[a,d]-5-环庚酮的合成新方法[J]. 中国药物化学杂志, 2006, 16(1): 49-50,53 |
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| 作者姓名： | 谢艳 吾国强 郑土才 陈芬儿 |
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| 作者单位： | 1. 衢州学院,化工系,浙江,衢州,324006
2. 复旦大学,化学系,上海,200043 |
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| 摘 要： | 以2-氰基一3一甲基吡啶为原料，通过自由基反应、Wittig-Homer反应、水解、还原、环化反应合成氯雷他定的重要中间体8-氯-10，11-二氢-4-氮杂-5H-二苯并[a，d]-5-环庚酮，总收率为20％。其结构经元素分析、核磁共振、质谱确证。
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| 关 键 词： | 药物化学 工艺改进 化学合成 氯雷他定 8-氯-10,11-二氢-4-氮杂-5H-二苯并[a,d]-5-环庚酮 |
| 文章编号： | 1005-0108（2006）01-0049-02 |
| 收稿时间： | 2005-07-18 |
| 修稿时间： | 2005-07-18 |
New method for the synthesis of 8-chloro-10,11-dihydro-4-aza-5H-dibenzo[a,d]cyclohepten-5-one |
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| XIE Yan,WU Guo-qiang,ZHENG Tu-cai,CHEN Fen-er. New method for the synthesis of 8-chloro-10,11-dihydro-4-aza-5H-dibenzo[a,d]cyclohepten-5-one[J]. Chinese Journal of Medicinal Chemistry, 2006, 16(1): 49-50,53 |
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| Authors: | XIE Yan WU Guo-qiang ZHENG Tu-cai CHEN Fen-er |
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| Affiliation: | 1. Department of Chemistry, Quzhou College, Quzhou 324006, China; 2. Department of Chemistry, Fudan University, Shanghai 200043, China |
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| Abstract: | A new synthetic method of 8-chloro-10, l l-dihydro-4-aza-5H-dibenzo[a, d] cyclohepten-5-one, an important intermediate of loratadine, was reported. Using 2-cyano-3-methylpyrldine as the starting materi al, through radical reaction, Wittig-Horner reaction, hydrolysis, reduction and cyclization it was synthesized. The total yield was 20 %. The chemical structure was analysis. confirmed by means of ^1H NMR, MS and elementary |
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| Keywords: | medicinal chemistry process improvement chemical synthesis loratadlne 8-chloro- 10, 11-dihydro-4-aza-5 H-dibenzo[ a, d] cyclohepten-5-one |
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