2-氟中氮茚衍生物的合成及表征

Syntheses and Characterization of 2-Fluoroindolizine Derivatives

2,2-二氟乙烯基对甲苯磺酸酯(2)与吡啶和异喹啉的叶立德(3)在DMF溶剂中,以K2CO3与Et3N作为混合碱,70 ℃条件下通过1,3-偶极反应24 h,以50%～70%的产率合成得到2位单氟环加成产物,2-氟中氮茚及2-氟苯并中氮茚衍生物4.通过红外光谱、核磁共振氢谱、氟谱、质谱和元素分析测试对该系列化合物进行了结构确认,并探讨了反应机理.

Fluoroindolizines and 2 fluoro benzo\indolizines 4 were synthesized in yields of 50%~70% via a 1,3 dipolar reaction of fluorinated vinyl tosylate 2 with N ylides of pyridinium or isoquinolinium for 24 h in the presence of K 2CO 3 and Et 3N in DMF. Their structures were confirmed by 1 H NMR, 19 F NMR, IR, MS and elemental analyses. A reaction mechanism is proposed.