| 三尖杉碱吲哚类似物的全合成 |
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| 引用本文： | 张强,闻韧,Henin J,Laronze JY.三尖杉碱吲哚类似物的全合成[J].复旦学报(医学版),2000,27(3):157-162. |
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| 作者姓名： | 张强 闻韧 Henin J Laronze JY |
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| 作者单位： | 1. 上海医科大学药学院合成药物化学教研室上海 200032
2. 法国兰斯大学药学院兰斯 51096 |
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| 基金项目： | 国家自然科学基金项目(29872029)、上海市教委重点学科资助项目(98-12) |
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| 摘 要： | 目的合成三尖杉碱吲哚类似物。方法以色胺为原料经缩合、环合、水解与脱羧反应得吲哚哌啶酮化合物，经Bischler-Napieralski反应得烯胺。通过烯胺的溴化与氧化-重排反应得到吲哚氮杂
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| 关 键 词： | 三尖杉碱 三尖杉酯碱 三尖杉碱吲哚类似物 合成 |
| 修稿时间： | 1999年10月15 |
Total Synthesis of Indole Analogues of Cephalotaxine |
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| ZHANG Qiang,WEN Ren,Henin J,Laronze JY.Total Synthesis of Indole Analogues of Cephalotaxine[J].Fudan University Journal of Medical Sciences,2000,27(3):157-162. |
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| Authors: | ZHANG Qiang WEN Ren Henin J Laronze JY |
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| Abstract: | Purpose To synthesize indole analogues of cephalotaxine in order to find new anti tumor compound. Methods Two alkylations of diethyl malonate gave the disubstituted malonate,which condensed with tryptamine in presence of potassium carbonate afforded lactame.Bischler Napieralski reaction gave the enamine.After bromination and Duhamel's oxidative rearrangement,azepinone was prepared.The proton was protected by benzyl.Reduction of gave alcohol which underwent intramolecular cyclization in acidic medium leading to the pentacyclic ketone(indole analogues of cephalotaxine). Results Indole analogues of cephalotaxine was synthesized via 10 steps,the overall yield was 14.3%. Conclusions Indole analogues of cephalotaxine was synthesized,the reaction was improved and the yield was increased,the by product was reduced. |
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| Keywords: | cephalotaxine harringtonine indolcephalotaxine synthesis |
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