Abstract：
The high utility of halogenated organic compounds has prompted the development of numerous transformations that install the carbon-halogen motif. Halogen functionalities, deemed as \"functional and functionalizable\" molecules due to their capacity to modulate diverse internal properties, constitute a pivotal strategy in drug discovery and development. Traditional routes to these building blocks have commonly involved multiple steps, harsh reaction conditions, and the use of stoichiometric and/or toxic reagents. With the emergence of solid halogen carriers such as N-halosuccinimides, and halohydantoins as popular sources of halonium ions, the past decade has witnessed enormous growth in the development of new catalytic strategies for halofunctionalization. This review aims to provide a nuanced perspective on nucleophilic activators and their roles in halogen activation. It will highlight critical discoveries in effecting racemic and asymmetric variants of these reactions, driven by the development of new catalysts, activation modes, and improved understanding of chemical reactivity and reaction kinetics.
摘要：
卤化有机化合物的高实用性促使了安装碳-卤素基序的许多转化的发展。卤素功能，由于其调节各种内部性质的能力，被认为是“功能性和可功能化的”分子，构成了药物发现和开发的关键战略。通往这些构建块的传统路线通常涉及多个步骤，苛刻的反应条件,以及使用化学计量和/或有毒试剂。随着N-卤代琥珀酰亚胺等固体卤素载体的出现，和卤海内酰脲作为卤离子的流行来源，在过去的十年中，在开发用于卤素官能化的新催化策略方面取得了巨大的增长。这篇综述旨在提供关于亲核活化剂及其在卤素活化中的作用的细微差别的观点。它将突出实现这些反应的外消旋和不对称变体的关键发现，在新催化剂开发的推动下，激活模式,并提高了对化学反应性和反应动力学的理解。
