欢迎访问过程工程学报, 今天是

›› 2006, Vol. 6 ›› Issue (6): 912-916.

• 过程与工艺 • 上一篇    下一篇

10-羟基喜树碱水溶性磷酰化衍生物的合成

杨柳,徐春艳,贾梦秋   

  1. 北京化工大学材料科学与工程学院
  • 出版日期:2006-12-20 发布日期:2006-12-20

Synthesis of New Water-soluble 10-Hydroxycamptothecin Derivative

YANG Liu,XU Chun-Yan,JIA Meng-Qiu   

  1. College of Materials Science and Engineering, Beijing University of Chemical Technology
  • Online:2006-12-20 Published:2006-12-20

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0.01 mol HCPT),反应温度-10℃,搅拌下反应时间30 min;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1.5 h;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%.

关键词: 10-羟基喜树碱, 磷酰化, 合成, 衍生物

Abstract: Water-soluble derivative with the lactone ring intact was synthesized by using 10-hydroxycamptothecin (HCPT) as raw material and pyridine as solvent through phosphorylation, esterification and hydrolysis. The optimal reaction conditions for the phosphorylation were determined as follows: n(POCl3):n(HCPT)=2:1 (based on 0.01 mol HCPT), the reaction temperature -10℃, and the reaction time 30 min under stirring, for the esterification 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-hydroxycamptothecin derivative, was separated by octodecyl silica gel preparative column. The total yield of the derivative was 30%.

Key words: 10-hydroxycamptothecin, phosphorylation, synthesis, derivative