Six amphiphilic cholesterylated thiogalactosides la-f with high affinity for the asialoglycoprotein receptor have been synthesized by coupling 2,3,4,6-tetra -O-acetyl-l-thio-β-D-galactopyranose 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.