Recent Advances in N-Arylation of Heterocycles in the Past Decade

Abstract

N-arylated heterocycles are a significant class of core scaffolds in medicinal chemistry, materials science, and agrochemistry, highlighting their importance in various fields. The development of innovative methodologies for synthesizing these fundamental structures has been a central focus in organic synthesis. Over the past few decades, numerous approaches have been established to synthesize N-aryl heterocycles efficiently. Among these methods, the direct N-arylation of N-H heterocycles stands out as one of the most straightforward and robust strategies for accessing N-arylated heterocycles. This review provides a comprehensive review of the recent advances in the synthesis of N-arylated heterocycles, encompassing the relevant literature from the past decade. The review summarizes the N-arylation of N-H heterocycles using various catalytic systems, including palladium, nickel, copper, visible light-induced metal-catalyzed, and metal-free catalyzed methodologies. These advances highlighted the continuous evolution and optimization of synthetic strategies to create diverse and complex N-arylated heterocycles, which are pivotal for furthering research and development in multiple scientific domains.