5-对羧基苯基-10,15,20-三间羟基苯基二氢卟吩-PEG-叶酸的设计与合成  

Design and Synthesis of 5-(4-Carboxyphenyl)-10,15,20-tris(3-Hydroxyphenyl)chlorin-PEG-Folic Acid

作　　者：李鹏熙[1] 郭林峰[2] 李东红[1] 

机构地区：[1]创伤烧伤复合伤国家重点实验室第三军医大学大坪医院野战外科研究所第二研究室,重庆400042 [2]西华师范大学化学化工学院,四川南充637002

出　　处：《精细化工中间体》2012年第6期22-25,共4页Fine Chemical Intermediates

基　　金：国家自然科学基金资助项目(21072227)

摘　　要：以聚乙二醇二胺、叶酸、5-对羧基苯基-10,15,20-三间羟基苯基二氢卟吩为原料,合成了2个光敏化合物:5-对羧基苯基-10,15,20-三间羟基苯基二氢卟吩-PEG-叶酸(3a)和5-对羧基苯基-10,15,20-三间羟基苯基二氢卟吩-PEG-NHBoc(3b),其结构经UV、IR、HPLC、1H MNR和MS确认。采用L9(33)正交实验法优化目标物3a的合成条件,在n(DCC)∶n(卟吩)=2∶1、反应温度为50℃、反应时间为5d时,3a收率最好。5-(4-Carboxyphenyl)-10,15,20-tris(3-hydroxyphenyl)chlorin-PEG-Folic acid and 5-(4 carboxyphenyl)-10,15,20-tris(3-hydroxyphenyl)chlorin-PEG-NH-Boc were synthesized starting from poly(ethylene glycol)-diamine,folic acid and 5-(4-carboxyphenyl)-10,15,20-tris(3-hydroxyphenyl)chlorin.The structures of the target compounds were characterized by UV-Vis,IR,HPLC,1HNMR and MS spectra.The synthesis condition of target compound 3a was investigated by L9(33) orthogonal experiment,and found that the yield of compound 3a was the highest as the molar ratio of DCC to chlorin was 2∶1,temperature was 50℃ and reaction time was 5 d.

关 键 词：光敏剂 二氢卟吩 叶酸 聚乙二醇二胺 

分 类 号：O625.6[理学—有机化学]