| 常山酮的合成方法研究 |
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| 引用本文： | 顾艳艳,刘世旭,王诗玺,万升标,江涛.常山酮的合成方法研究[J].中国海洋大学学报(自然科学版),2011,41(9):67-70. |
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| 作者姓名： | 顾艳艳 刘世旭 王诗玺 万升标 江涛 |
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| 作者单位： | 中国海洋大学医药学院教育部海洋药物重点实验室,山东青岛,266003 |
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| 基金项目： | 青岛市科技攻关计划(08-2-4-4-nsh); 科技部科技人员服务企业计划(2009GJC60017)资助 |
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| 摘 要： | 本文对常山酮(halofuginone)的合成方法进行了研究和改进,以2-甲基-3-羟基吡啶为起始原料,其甲基化产物与乙腈加成后经Rh/Al2O3选择性还原得(3-甲氧基-2-哌啶基)-丙酮,再经溴代、N-保护后与6-氯-7-溴-4(3H)-喹唑啉酮偶联,产物经水解脱保护得目标化合物6-氯-7-溴-3-(3-(3-羟基-2-哌啶基)-丙酮基)-4(3H)-喹唑啉酮氢溴酸盐,通过6步反应制得了常山酮,总收率为11.6%,为常山酮的工业化生产提供了可能。目标产物和各步中间体结构经MS1、H NMR和13CNMR确证。
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| 关 键 词： | 常山酮 抗球虫药 合成方法 |
Study on the Synthetic Technique of Halofuginone |
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| GU Yan-Yan,LIU Shi-Xu,WANG Shi-Xi,WAN Sheng-Biao,JIANG Tao.Study on the Synthetic Technique of Halofuginone[J].Periodical of Ocean University of China,2011,41(9):67-70. |
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| Authors: | GU Yan-Yan LIU Shi-Xu WANG Shi-Xi WAN Sheng-Biao JIANG Tao |
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| Institution: | GU Yan-Yan,LIU Shi-Xu,WANG Shi-Xi,WAN Sheng-Biao,JIANG Tao(The Key Laboratory of Marine Drugs,Ministry of Education,College of Medicine and Pharmacy,Ocean University of China,Qingdao 266003,China) |
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| Abstract: | The synthesis of Halofuginone was researched and improved in this artical.Halofuginone was synthesized from 2-methylpyridin-3-ol by methylation addition and selective catalytic reduction to give 1-(3-methoxypiperidin-2-yl)propan-2-one,which was subjected to bromination,N-protection,substitution to afford allyl 2-(3-(7-bromo-6-chloro-4-oxo-quinazolin-3(4H)-yl)-2-oxopropyl)-3-methoxypiperidine-1-carboxylate,and finally hydrolation with acid to give the product.The chemical structures of halofuginone and its i... |
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| Keywords: | halofuginone anti-coccidiosis synthetic method |
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