Heteroarenes containing oxygen, nitrogen, and/or sulfur are important in numerous aspects of chemistry and everyday life. C–H functionalization of heteroarenes represents the fastest and most atom-economical approach for the synthesis of complex molecules. This strategy avoids the requirement of de novo synthesis and is beneficial for the late-stage modification of structurally complex molecules. Although early protocols for C–H functionalization using organic halides (I, Br, and Cl) as coupling partners remain in active use today, a range of modern strategies allows the cleavage of less reactive C–Het (F, O, S, N, and P) and C–C bonds to form essential links to the feedstock chemicals, highlighting their renewable and sustainable features. This review focuses on modern strategies for the C–H functionalization of heteroarenes with these alternative coupling partners. Most of the transformations can be achieved through catalytic processes. Some non-catalytic strategies involving new reagents and techniques are also introduced.

含氧、氮和/或硫的杂芳烃在化学和日常生活的许多方面都很重要。杂芳烃的 C-H 官能化代表了合成复杂分子的最快和最原子经济的方法。这种策略避免了从头开始的要求合成，有利于结构复杂分子的后期修饰。尽管使用有机卤化物（I、Br 和 Cl）作为偶联伙伴的 C-H 功能化的早期方案今天仍在积极使用，但一系列现代策略允许裂解反应性较低的 C-Het（F、O、S、N 、P) 和 C-C 键形成与原料化学品的重要联系，突出其可再生和可持续的特征。本综述侧重于用这些替代偶联伙伴对杂芳烃进行 C-H 功能化的现代策略。大多数转化可以通过催化过程实现。还介绍了一些涉及新试剂和技术的非催化策略。