9-硝基喜树碱酯类衍生物的合成和结构表征  

Synthesis and Characterization of 9-nitrocamptothecin C-10 Esters

作　　者：牟璠松[1] 罗猛[1] 付玉杰[1] 张谡[1] 祖元刚[1] 

机构地区：[1]森林植物生态学教育部重点实验室(东北林业大学),哈尔滨150040

出　　处：《东北林业大学学报》2010年第1期74-75,83,共3页Journal of Northeast Forestry University

基　　金：国家自然科学基金项目(30770231);黑龙江省杰出青年科学基金项目(JC200704);黑龙江省自然科学基金项目(C200933);东北林业大学青年科研基金项目(07021)

摘　　要：以10-羟基喜树碱为原料,经硝化反应制备中间体9-硝基-10-羟基喜树碱,再经亲核取代反应合成新的9-硝基喜树碱酯类衍生物。对反应路线的选择及反应中间体和终产物的结构进行了详细解析,化合物的结构经1HNMR、13C NMR、IR和MS(ESI)表征。结果表明:此合成路线反应条件温和,产物总转化率达到90.2%。A study was conducted to synthesize 9-nitrocamptothecin C-10 esters in order to find out a new type of camptothecin prodrug with low toxicity.10-hydroxycamptothecin was used as raw material to prepare 9-nitro-10-hydroxycamptothecin by nitration,and then two new 9-nitrocamptothecin ester derivatives were synthesized by nucleophile substitution with ethyl bromoacetate.The selection of synthetic route and the structure of the final products were discussed in detail.The structure of each compound was characterized by 1H NMR,13C NMR,IR and MS（ESI）.Results indicate that the selected synthetic route is easy to perform under mild conditions,and the maximum yield of the final products reached 90.2%.

关 键 词：9-硝基喜树碱 酯类衍生物 亲核取代反应 

分 类 号：R914.5[医药卫生—药物化学]