含氟取代蝶啶类化合物的合成及结构表征

Synthesis and Characterization of Pteridine Derivatives with Fluorine-contained Groups

目的合成一系列6-含氟烷氧基蝶啶类化合物并确证其化学结构。方法以3-氨基吡嗪-2-羧酸甲酯为起始底物,通过氨化、卤代、合环等六步反应合成一系列6-含氟烷氧基蝶啶类化合物。测定目标化合物的物理常数,并通过多种波谱分析技术(核磁共振氢谱、红外光谱、质谱)对其结构进行表征。结果以较高的产率(六步反应的总产率均大于24. 7%)制备多种6-含氟烷氧基蝶啶类化合物,经核磁共振氢谱及质谱等多种波谱手段确证为目标化合物。结论该方法操作简便,产率稳定,为未来的抗肿瘤活性实验提供有力的支持。

OBJECTIVE A series of 6-fluorine-contained alkoxyl pteridinesderivatives have been synthesized and their structures have been characterized. METHODS With methyl 3-aminopyrazine-2-carboxylate as the starting material,a series of 6-fluorine-contained alkoxyl pteridines derivatives have been yielded through 6 steps reaction involving amination,halogenationand cyclization etc.The physical constants of target compounds were determined,and their structures were characterized using various spectra techniques （1H-NMR,IR,MS）. RESULTS 6-fluorine-contained alkoxyl pteridinesderivatives were prepared with a relatively higher yield （total yields for 6 steps reaction were higher than 24.7%）,which were proved as target compounds byusing various spectra techniques such as 1H-NMR and MS etc. CONCLUSIO The synthetic route,with simple processes and good yields,substantially supports the antitumor study in the future.