Study on synthesis and distribution in vivo of 5-Fu-cholic acid conjugate  

作　　者：Jie Li Li Hai Wei Jia Liu Xiao Chun Wu Yong Wu 

机构地区：[1]Key Laboratory of Drug Targeting of Education Ministry, West China School of Pharmacy, Sichuan University Chengdu 610041, China [2]Sichuan Normal University, Chemistry and Material College, Chengdu 610066, China

出　　处：《Chinese Chemical Letters》2009年第2期136-138,共3页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.30672537);Special Research Fund for Dr.discipline Sites of Colleges and Universities(No.20050610085).

摘　　要：A series of hepatic targeting drugs, 5-Fu-cholic acid conjugate T1-T5, were synthesized. 5-Fu and cholic acid was selected as starting material, after N-hydroxymethylation, condensation, hydrogenolysis to obtain carboxylated 5-Fu 5a-e. Carboxylated 5-Fu 5a-e were condensated with intermediate 3-hydroxyethyl cholic acid benzyl ester 6 to get 7a-e, 7a-e were deprotected to get T1- T5.A series of hepatic targeting drugs, 5-Fu-cholic acid conjugate T1-T5, were synthesized. 5-Fu and cholic acid was selected as starting material, after N-hydroxymethylation, condensation, hydrogenolysis to obtain carboxylated 5-Fu 5a-e. Carboxylated 5-Fu 5a-e were condensated with intermediate 3-hydroxyethyl cholic acid benzyl ester 6 to get 7a-e, 7a-e were deprotected to get T1- T5.

关 键 词：Hepatic targeting drugs Cholic acid SYNTHESIS 

分 类 号：TQ464.54[化学工程—制药化工] TN821.8[电子电信—信息与通信工程]