食品与药品
食品與藥品
식품여약품
FOOD AND DRUG
2012年
11期
388-389
,共2页
替加氟%1,3,4-噻二唑%合成
替加氟%1,3,4-噻二唑%閤成
체가불%1,3,4-새이서%합성
ftorafur%1,3,4-thiadiazol%synthesis
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.
目的探索高效低毒的抗腫瘤藥物.方法替加氟(FT-207)為先導化閤物,經取代反應、水解反應製得N1-(四氫-2-呋喃基)-N3-乙痠基-5-Fu,在N,N,-二環己基碳酰亞胺(DCC)作用下分彆與2-氨基-1,3,4-噻二唑及2-氨基-5-甲基-1,3,4-噻二唑反應,生成目標化閤物M1及M2.結果 M1及M2結構經紅外光譜、質譜、元素分析和覈磁共振氫譜確證.結論閤成路線閤理,操作簡便,值得進一步研究.
목적탐색고효저독적항종류약물.방법체가불(FT-207)위선도화합물,경취대반응、수해반응제득N1-(사경-2-부남기)-N3-을산기-5-Fu,재N,N,-이배기기탄선아알(DCC)작용하분별여2-안기-1,3,4-새이서급2-안기-5-갑기-1,3,4-새이서반응,생성목표화합물M1급M2.결과 M1급M2결구경홍외광보、질보、원소분석화핵자공진경보학증.결론합성로선합리,조작간편,치득진일보연구.
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.
