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 novel bifunctional glycolipid which carded a cluster of thiogalactosides as the hepatocyte targeting ligand for gene delivery was prepared. Hexa-antennary alcohol 1 was used as the core scaffold to attach a cholesterol molecule by a poly（ethylene glycol） chain, while its remaining branches were linked with five acetylgalactosides, which would be deacetylated later to produce pentaantennary galactoside. Liposome containing the galactoside showed high affinity and transfection activity in hepatoma cells HepG2.
Qing Lin Jiang Li Hai Lei Chen Jiao Lu Zhi Rong Zhang Yong Wu
A novel bifunctional compound carrying duster thiogalactoside as the cell targeting ligands was synthesized for gene delivery to hepatocytes. Tetra-antennary dendr-OMs4 5 was used as a scaffold for the attachment of three galactosides, while the other mesylate end was linked with cholesterol through poly（ethylene glycol） chain. This design provided an effective entry for the synthesis of the bifunctional compound.
Lei Tang Yong Wu Jiao Lu Zhi Rong Zhang Jin Cheng Yang Li Hai
Tilisolol hydrochloride 1, a non-selective β-adrenoceptor blocker, was developed as a drug for the treatment of hypertension and angina pectoris. The optical active forms of 1, la and lb were synthesized from inexpensive phthalic anhydride 2 in eight steps with 13% （S） and 15% （R） overall yield.
