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| 紫杉醇合成中的脱氧反应 | |
| 引用本文： | 王淑萍,顾军,程虹. 紫杉醇合成中的脱氧反应[J]. 武警医学院学报, 2009, 18(4): 283-285 |
| 作者姓名： | 王淑萍 顾军 程虹 |
| 作者单位： | 1. 武警医学院附属医院药剂科,天津,300162 2. 武警医学院药物化学教研室,天津,300162 3. 武警医学院附属医院护理部,天津,300162 |
| 基金项目： | 武警医学院博士启动基金 |
| 摘 要： | 【目的】探讨紫杉醇类化合物合成中的脱氧反应新方法。【方法】由偶氮二异丁腈引发30％过氧化氢产生自由基，以链式自由基反应机制脱除紫杉醇类化合物结构中的含氧基团。【结果】通过自由基反应历程以30％过氧化氢高效率地去除了底物结构中的羟基，收率达到84％。对于含有末端双键结构的底物，应加入环己烯作为“牺牲剂”以提高反应收率。【结论】此方法简单、高效、实用，毒性低，适合较大规模反应。 |
| 关 键 词： | 脱氧反应 紫杉醇 合成 过氧化氢 |
Deoxygenation in the synthesis of taxol |
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| WANG Shu-ping,CHENG Hong,GU Jun. Deoxygenation in the synthesis of taxol[J]. Acta Academiae Medicinae CPAPF, 2009, 18(4): 283-285 | |
| Authors: | WANG Shu-ping CHENG Hong GU Jun |
| Affiliation: | (Department of Pharmacy, Medical College of Chinese People＇s Armed Porice Force, Tianjin 300162, China) |
| Abstract: | [Objective] To investigate the new method of deoxygenation in the synthesis of taxol. [Methods] Chain deoxygenation method by radicals generated from 30% hydrogen peroxide induced by azodiisobutyronitrile was firstly used in the synthesis of taxol to remove the hydroxyl group. [ Results] Deoxygenation yield of reaction was high up to 84% by radical mechanism. Sacrificial agent should be added to the system to increase the reaction yield if terminal double - bond structure exist. [Conclusions] This deoxygenation is an efficient, non-toxic, simple and scall-up method in the synthesis of taxol. |
| Keywords: | Deoxygenation Taxol Synthesis Hydrogen peroxide |
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