正交实验设计优化光敏剂二氢卟吩e_6的合成工艺  

Optimization of synthesis of photosensitizer chlorin e_6 by orthogonal design

作　　者：马福家[1] 姚建忠[1] 张万年[1] 余建鑫[1] 章玲[1] 盛春泉[1] 宋云龙[1] 缪振元[1] 张珉[1] 

机构地区：[1]第二军医大学药学院,上海200433

出　　处：《中国药学杂志》2005年第20期1589-1591,共3页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金(30371737)

摘　　要：目的优化光敏剂二氢卟吩e6(1)的合成工艺.方法按L9(34)正交表设计考察了影响以脱镁叶绿酸a(2)为原料合成二氢卟吩e6产率的回流反应时间(A)、氢氧化钾溶液浓度(B)、溶剂(C)和投料比(D)4个主要因素,每个因素各取3个水平.结果合成1的最优反应条件为B1A3C2D2,反应工艺收率从50.6%提高到58.1%.结论新工艺提高了收率、缩短了反应时间、消除了毒性溶剂,适合工业化生产.OBJECTIVE To optimize the synthesis of photosensitizer chlorin e6 （1）. METHODS Target compound 1 was synthesized through the alkali reflux reaction of pheophorbide a（2） which was preduced by the acidic degradation of silkworm excrement crude chlorophyll extracts. Four main factors influencing synthetic yield of 1, such as reflux time（A）, the concentration of potassium hydroxide（B）, solvent（C） and the weight ratio of material 2 to potassium hydroxide （ D）, each being choosed three levels, were evaluated by the orthogonal experimental design of L9（3^4） .RESULTS The optimization terms of the synthesis of target compound 1 were B1A3C2D2. The yield of 1 was raised from 50.6 % to 58.1%. CONCLUSION The yield is raised, and the reaction time is shortened and the toxic solvent is removed. The procedure, developed is suitable for industrial preduction.

关 键 词：药物化学 工艺改进 化学合成 二氢卟吩e6 正交设计 光敏剂 

分 类 号：R914.5[医药卫生—药物化学]