呋喃氟尿嘧啶衍生物M_1、M_2的合成  

Synthesis of Ftorafur Derivative M_1 and M_2

作　　者：刘爱芹[1] 于胜海[1] 

机构地区：[1]山东省医学科学院药物研究所,山东济南250062

出　　处：《食品与药品》2012年第11期388-390,共3页Food and Drug

基　　金：山东省自然科学基金项目(ZR2010HM064)

摘　　要：目的探索高效低毒的抗肿瘤药物。方法替加氟(FT-207)为先导化合物,经取代反应、水解反应制得N1-(四氢-2-呋喃基)-N3-乙酸基-5-Fu,在N,N,-二环己基碳酰亚胺(DCC)作用下分别与2-氨基-1,3,4-噻二唑及2-氨基-5-甲基-1,3,4-噻二唑反应,生成目标化合物M1及M2。结果 M1及M2结构经红外光谱、质谱、元素分析和核磁共振氢谱确证。结论合成路线合理,操作简便,值得进一步研究。Objective To obtain an antitumor drug with high activity and low toxicity. Methods With ftorafur as lead compound, N1-（tetrahydrofuran-2-yl）-N3-acetoxy-5-fluorouracil was synthesized by substitution reaction and hydrolysis reaction, then coupled in the existence of DCC with 2- amine-1,3,4-thiadiazol and 5-methyl-2- amine-1,3,4- thiadiazol respectively, to produce target M1 and M2. Results The structures of target M1 and M2 were identified by IR, HPLC-MS, elemental analysis and 1H-NMR. Conclusion The synthetic route can be rational and simple, and is worth further development.

关 键 词：替加氟 1 3 4-噻二唑 合成 

分 类 号：R914.5[医药卫生—药物化学]