6-氮杂脲嘧啶类化合物C-H键官能化反应研究进展  

Research Advancements on the C-H Bond Functionalization of 6-azauracils

作　　者：石伟烁 屈凌波[1,2] 景珺 樊璐露 SHI Weishuo;QU Lingbo;JING Jun;FAN Lulu(School of Chemistry&Chemical Engineering,Henan University of Technology,Zhengzhou 450001,China;School of Chemical Engineering,Zhengzhou University,Zhengzhou 450001,China)

机构地区：[1]河南工业大学化学化工学院,河南郑州450001 [2]郑州大学化工学院,河南郑州450001

出　　处：《山东化工》2025年第5期106-111,共6页Shandong Chemical Industry

基　　金：河南省自然科学基金青年基金(242300421617)。

摘　　要：6-氮杂脲嘧啶是一种重要的六元杂环化合物,它由尿嘧啶6号位的C原子被N原子取代所得,是尿嘧啶的一种类似物。6-氮杂脲嘧啶骨架是多种生物活性分子的基本结构单元,其衍生物常具有特殊的药理和生理活性,对其骨架修饰的研究获得了合成化学家的持续关注。6-氮杂脲嘧啶的骨架修饰研究多集中在杂环的氮原子上和环上C-H键的官能化方面,涉及的反应包括氮上的亲核取代反应,C-H键的烷基化、酰化、芳化等。C-H键的官能化反应一直是有机合成化学研究的热点,其是在不破坏原有分子骨架的基础上,通过直接在C-H键上引入官能团来合成新的化合物。6-氮杂脲嘧啶类化合物作为重要的生物活性分子,其C-H键官能化反应对于合成新型药物分子具有重要意义。本文主要对近年来6-氮杂脲嘧啶类化合物C5位上的C-H键的官能化反应进行综述,并对其研究方向进行展望。6-azauracil is an important six-membered heterocyclic compound.Structurally,it is derived from uracil by substituting the carbon atom at position 6 with a nitrogen atom,making it an analogue of uracil.The 6-azauracil skeleton serves as a fundamental structural unit in various bioactive molecules,and its derivatives often exhibit unique pharmacological and physiological activities.Thus,the research on the modification of its framework has garnered continuous attention from synthetic chemists.The studies on the skeleton modification of 6-azauracil mainly focus on the nitrogen atoms in the heterocycle and the functionalization of the C-H bond on the heterocyclic ring.The reactions involved nucleophilic substitutions at nitrogen atoms,as well as C-H bond alkylation,acylation,arylation,etc.The functionalization of C-H bonds has been a hot topic in synthetic organic chemistry,as it allows to synthesize new compounds by directly introducing functional groups onto C-H bonds without disrupting the original molecular framework.As important bioactive molecules,the C-H bond functionalization of 6-azauracils is of great significance for the synthesis of novel drug molecules.This article mainly reviews the C-H bond functionalization at the C5 position of 6-azauracils in recently years and looks forward to the future research directions.

关 键 词：6-氮杂脲嘧啶 C-H键官能化反应 尿嘧啶类似物 研究进展 

分 类 号：TQ254.1[化学工程—有机化工] O626.414[理学—有机化学]