7-溴吡咯-并[2,1-f][1,2,4]三嗪-4-胺的合成  

Synthesis of 7-Bromopyrrolo[2,1-f][1,2,4]triazin-4-amine

作　　者：郑军 曹国锐[1] ZHENG Jun;CAO Guo-rui(College of Chemical Engineering,Qingdao University of Science and Technology,Qingdao 266042,China)

机构地区：[1]青岛科技大学化工学院,山东青岛266042

出　　处：《化学试剂》2020年第5期608-611,共4页Chemical Reagents

摘　　要：吡咯并[2,1-f][1,2,4]三嗪类化合物作为抗肿瘤药的关键母核,其应用越来越广。以水合肼和二碳酸二叔丁酯为原料经酰化、Clauson Kaas吡咯合成、取代、脱保护、环化、溴化6步反应合成了标题化合物。6步反应总收率达到36%,化合物结构经1HNMR和MS确定。合成方法具有反应条件温和、易于操作、后处理方便和产率较高等优点。Pyrrolo[2,1-f][1,2,4]triazines are widely used as key nucleus for antitumor drugs.The title compound was synthesized from hydrazine hydrate and di-tert-butyl dicarbonate by acylation,Clauson Kaas,substitution,deprotection,cyclization and bromination.The total yield of 6 steps reaction reached 36%and the structure of the target molecules was confirmed by 1HNMR and MS.The synthesis method has the advantages of mild reaction conditions,easy operation,convenient post-treatment and high yield.

关 键 词：7-溴吡咯并[2 1-f][1 2 4]三嗪-4-胺 小分子抗癌药 关键母核 三嗪 医药中间体 合成 

分 类 号：O626.13[理学—有机化学]