| 李尚丰,马秀光,黄以军.化学通报,2017,80(12):1148-1151,1127. |
| 一类高喜树碱化合物的新型合成方法 |
| A New Synthetic Protocol for a Series of Novel Homocamptothecin Compounds |
| 投稿时间：2017-05-25 修订日期：2017-08-18 |
| DOI： |
| 中文关键词: 高喜树碱 拓扑异构酶 |
| 英文关键词:Homocamptothecin, topoisomerase |
| 基金项目:上海市科委科研计划项目(14431903000) |
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| 中文摘要: |
| 本文创造性地以溴乙酸叔丁酯与9-羟基喜树碱反应, 摈弃了磷酸酯等保护基团, 路线简洁, 收率提高, 既起到了提高喜树碱溶解度的作用, 便于后面反应的进行和产物纯化, 又引入了羧酸官能团, 能很方便地合成一系列高喜树碱酰胺化合物。 |
| 英文摘要: |
| A new protocol was developed to synthesize a series of novel homocamptothecin compounds starting from t-butyl bromoacetate in a creative way. This way is quite straightforward and simple and the gross yield makes a great improvement without the use of the reported phosphate or other traditional protective groups. It enhances the solubility of each camptothecin derivative, accelerates the reaction to completion and simplifies the workup and purification. As a result, a lot of amides could be ready to be got after amidation. |
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