摘要
Aseriesofglucose-cholesterolderivatives8a-8easligandsforbraintargetingliposomesweresynthesized.Thepreparationofcompound6involvedtemporaryprotectionofglucosewithchlorotrimethylsilicaneandhexamethyldisilazanefollowedbyselectivelyhydrolyzed.Theknowncholesteryltosylate1werecoupledtoethyleneglycolstoaffordalcohol2a-2e.Substitutionanddeprotectionofalcohol2a-2efurnishedtheacids4a-4e,whichwascondensedwithcompound6togetcompounds7a-7e,andthenwasdeprotectedintetrahydrofuranwithTFAtoobtainthetitlecompounds.Asamodeldrug,tegafurwasentrappedbyliposomescoupledwith8b,andpreliminaryinvivoevaluationshown8bcouldenhancetheabilityofliposomesdeliveringtegafuracrossthebloodbrainbarrier.
出版日期
2011年07月17日（中国期刊网平台首次上网日期，不代表论文的发表时间）
