硫胺素二硫化物类脑靶向药物载体的设计与合成  

Design and synthesis of thiamine disulfides as carriers for brain targeted delivery

作　　者：姚念[1] 樊维[1] 余永国[1] 吴勇[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2012年第2期115-117,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81072532);教育部优先资助领域项目(批准号:20110181130011)

摘　　要：目的设计并合成一系列硫胺素二硫化物类脑靶向药物载体。方法 2-(4-甲基噻唑-5-基)乙醇(Ⅰ)在不同溴代物的作用下,氮烷基化制成季铵盐(Ⅱ),该中间体经碱性开环后与烷基硫代硫酸钠(Ⅳ)反应即得到目标产物Ⅴ。结果与结论成功制备了9个含有不同取代基的硫胺素二硫化物;目标化合物经1HNMR和MS确证。OBJECTIVE To synthesize a series of thiamine disulfides as carriers for brain targeted delivery.METHODS 2-（4-methylthiazol-5-yl）ethanol（Ⅰ） was treated with different alkyl bromides,leading to the quaternary ammonium salt（Ⅱ） by alkyl group substitution an nitrogen subsequently,intermediate Ⅱ was hydrolyzed and reacted with thiosulfate salts（Ⅳ） to furnish target compounds Ⅴ.RESULTS Nine thiamine disulfides with different substituents were designed and synthesized.CONCLUSION The chemical structures of the target compounds were confirmed by 1HNMR and MS.

关 键 词：脑靶向 硫胺素二硫化物 载体 合成 

分 类 号：R914[医药卫生—药物化学]