10-羟基喜树碱水溶性磷酰化衍生物的合成  

Synthesis of New Water-soluble 10-Hydroxycamptothecin Derivative

作　　者：杨柳[1] 徐春艳[1] 贾梦秋[1] 

机构地区：[1]北京化工大学材料科学与工程学院,北京100029

出　　处：《过程工程学报》2006年第6期912-916,共5页The Chinese Journal of Process Engineering

摘　　要：以10-羟基喜树碱(HCPT)为原料,吡啶为溶剂,经过磷酰化、酯化、水解三步反应合成了全新的水溶性磷酰化衍生物.得到的较佳工艺条件为:磷酰化反应三氯氧磷与HCPT的投料摩尔比2:1(相对0.01molHCPT),反应温度-10℃,搅拌下反应时间30min;酯化反应乙醇与HCPT的投料摩尔比6:1,反应温度10℃,搅拌下反应时间1.5h;水解反应保持体系pH<5.0.ODS制备柱分离得到产物,总收率为30.0%.Water-soluble derivative with the lactone ring intact was synthesized by using 10-hydroxyeamptotheein （HCPT） as raw matearial and pyridine as solvent through phosphorylation, esterification and hydrolysis. The optimal reaction conditions for the phosphorylation were determined as follows： n（POCl℃3）：n（HCPT）-2：1 （based on 0.01 tool HCPT）, the reaction temperature -10℃, and the reaction time 30 rain under stirring, for the estefification they are： n（ethanol）：n（HCPT）-6：1, the reaction temperature 10℃, and the reaction time 1.5 h under stirring pH〈5.0 in hydrolysis reaction. The product, 10-hydroxyeamptotheein derivative, was separated by octodeeyl silica gel preparative column. The total yield of the derivative was 30%.

关 键 词：10-羟基喜树碱 磷酰化 合成 衍生物 

分 类 号：R979.19[医药卫生—药品]