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

作　　者：林锦 陈振东 王艰[1] 许秀枝[1] 李柱来[1] LIN Jin;CHEN Zhen-dong;WANG Jian;XU Xiu-zhi;LI Zhu-lai ＊(Department of Pharmaceutical Chemistry,School of Pharmacy,Fujian Medical University,Fuzhou 350122,China)

机构地区：[1]福建医科大学药学院药物化学系,福州350122

出　　处：《海峡药学》2018年第10期84-86,共3页Strait Pharmaceutical Journal

摘　　要：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.

关 键 词：蝶啶 合成 表征 含氟 

分 类 号：R917[医药卫生—药物分析学]