A series of glucose-cholesterol derivatives 8a-8e as ligands for brain targeting liposomes were synthesized.The preparation of compound 6 involved temporary protection of glucose with chlorotrimethylsilicane and hexamethyldisilazane followed by selectively hydrolyzed.The known cholesteryl tosylate 1 were coupled to ethylene glycols to afford alcohol 2a-2e.Substitution and deprotection of alcohol 2a-2e furnished the acids 4a-4e,which was condensed with compound 6 to get compounds 7a-7e,and then was deprotected in tetrahydrofuran with TFA to obtain the title compounds.As a model drug,tegafur was entrapped by liposomes coupled with 8b,and preliminary in vivo evaluation shown 8b could enhance the ability of liposomes delivering tegafur across the blood brain barrier.