Six amphiphilic cholesterylated thiogalactosides 1a-f with high affinity for the asialoglycoprotein receptor have been synthesized by coupling 2,3,4,6-tetra -O-acetyl-1-thio-β-Dgalactopyranose 8 with prepared cholesterol derivatives 7a-f, then by deacetylating. Preliminary results show liposomes containing those galactosides derivatives exhibited higher affinity and transfection activity in hepatoma cells HepG2 and SMMC-7721.