抗癌药物紫杉醇的手性C_(13)侧链的合成  

Synthesis of the Taxol C_(13) Side Chain

作　　者：王巧峰[1] 姜茹[1] 孙晓莉[1] 程司堃[1] 陈雷 

机构地区：[1]中国人民解放军第四军医大学药学系化学教研室,陕西西安710032

出　　处：《解放军药学学报》2005年第3期198-200,共3页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金：国家自然科学基金项目;No.20272082;20302014

摘　　要：目的方便快捷的合成抗癌药物紫杉醇的C13侧链。方法以一种可回收的小分子手性配体催化反式肉桂酸乙酯的不对称二羟化(AD)反应,得到手性连二醇,产物再经两步反应可获得高光学活性的紫杉醇C13侧链。结果各步反应产品纯化方法简单,配体可重复使用,紫杉醇侧链产率48.4%。结论该方法显著降低了紫杉醇的生产成本,为工业化生产抗癌药物紫杉醇打下基础。Aim To synthesize C(13) side chain of taxol by a simple way.Method The chiral taxol side chain was prepared from asymmetric dihydroxylation (AD) of ethyl cinnamate which was catalyzed by OSO4 and a kind of recoverable ligand.Results The C(13) side chain of taxol was obtained with the total yield of 48.4% and high enantioselectivity.Conclusion The way to synthesize the C(13) side chain is so convenient and practical that it is of economic significance to produce taxol side chain in a large scale with low cost.

关 键 词：抗癌药物 合成 紫杉醇侧链 工业化生产 手性配体 光学活性 纯化方法 生产成本 反应 不对称 肉桂酸 小分子 

分 类 号：R979.1[医药卫生—药品] R284.3[医药卫生—药学]