Citation: Jie Li, Li Hai, Wei Jia Liu, Xiao Chun Wu, Yong Wu. Study on synthesis and distribution in vivo of 5-Fu-cholic acid conjugate[J]. Chinese Chemical Letters, ;2009, 20(2): 136-138. doi: 10.1016/j.cclet.2008.11.004 shu

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

Jie Li ^a, ,
Li Hai ^a ,
Wei Jia Liu ^a ,
Xiao Chun Wu ^b ,
Yong Wu ^a

a Key Laboratory of Drug Targeting of Education Ministry, West China School of Pharmacy, Sichuan University Chengdu 610041, China;
b Sichuan Normal University, Chemistry and Material College, Chengdu 610066, China

Received Date: 16 June 2008

Fund Project: This work was supported by the National Natural Science Foundation of China (No. 30672537) and Special Research Fund for Dr. discipline Sites of Colleges and Universities (No. 20050610085).

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.
- Hepatic targeting drugs,
- Cholic acid,
- Synthesis
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