6-苄氧基蝶啶类化合物的合成及结构表征  

Synthesis and Characterization of 6-benzyloxy Pteridine Derivatives

作　　者：林虔 杨康 许晴怡 黄学洋 林锦 李柱来[2] LIN Qian;YANG Kang;XU Qing-yi;HUANG Xue-yang;LIN Jin;LI Zhu-lai(Department of Pharmacy,People′s Hospital Affiliated to Fujian University of Traditional Chinese Medicine,Fuzhou 350004,China;Department of Pharmaceutical Chemistry,School of Pharmacy,Fujian Medical University,Fuzhou 350122,China;Public Health School,Fujian Medical University,Fuzhou 350122,China)

机构地区：[1]福建中医药大学附属人民医院药学部,福建福州350004 [2]福建医科大学药学院药物化学系,福建福州350122 [3]福建医科大学公共卫生学院,福建福州350122

出　　处：《海峡药学》2021年第6期72-75,共4页Strait Pharmaceutical Journal

摘　　要：目的制备多种6-苄氧基蝶啶结构衍生物并表征其化学结构。方法采用3-氨基吡嗪-2-羧酸甲酯作为初始底物,通过氨化、溴代、合环、苄氧基取代、氯代以及芳氨基化等六步反应合成一系列6-苄氧基蝶啶结构衍生物,并采用多种表征手段(核磁共振氢谱、红外光谱、质谱)对其结构进行确证。结果以较高的产率(六步反应的总产率均大于20%)制备一系列6-苄氧基蝶啶结构衍生物,通过核磁共振氢谱及质谱等多种有机波谱分析手段证实其为目标化合物。结论该方法操作简单,产率稳定,为之后的抗肿瘤实验提供有力支撑。OBJECTIVE A variety of 6-benzyloxy pteridines derivatives have been synthesized and their structures have been characterized.METHODS With methyl 3-aminopyrazine-2-carboxylate as the starting material,a series of 6-benzyloxy pteridines derivatives have been yielded through 6 steps reaction involving amination,bromination,cyclization,benzyloxylation,chlorination and arylamination etc.Their structures were characterized using various spectra techniques(1H-NMR,IR,MS).RESULTS 6-benzyloxy pteridines derivatives were prepared with a relatively higher yield(total yields for 6 steps reaction were higher than 20%),which were confirmed as target compounds by using various organic spectroscopy techniques such as 1H-NMR and MS etc.CONCLUSION The synthetic route,with simple processes and steady yields,would strongly support the subsequent antitumor studies.

关 键 词：蝶啶 合成 表征 苄氧基 

分 类 号：R917[医药卫生—药物分析学]