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

Jie Li Li Hai Wei Jia Liu Xiao Chun Wu Yong Wu

引用本文: 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
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

  • 基金项目:

    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).

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.

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  • 收稿日期:  2008-06-16
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