紫杉醇合成中的脱氧反应  

Deoxygenation in the synthesis of taxol

作　　者：王淑萍[1] 顾军[2] 程虹[3] 

机构地区：[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

出　　处：《武警医学院学报》2009年第4期283-285,共3页Acta Academiae Medicinae CPAPF

基　　金：武警医学院博士启动基金项目(WBS2008-03)

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。[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.

关 键 词：脱氧反应 紫杉醇 合成 过氧化氢 

分 类 号：R979.1[医药卫生—药品]