Multicomponent Synthesis of Alkyl BCP-Heteroaryls via Electron Donor–Acceptor Complex Photoactivation under Mild Conditions

In the vanguard of sustainable chemistry, the pursuit of efficient pathways for the synthesis of alkyl bicyclo[1.1.1]pentane-heteroaryls has captured the attention of the scientific vanguard. We herein report a groundbreaking and eco-conscious multicomponent coupling reaction that paves the way for the alkylation and heteroarylation of [1.1.1]propellane, a process uniquely enabled by the photochemical prowess of an electron donor–acceptor (EDA) complex. This method is distinguished by its minimalist yet powerful approach: devoid of transition metals, additives, and photosensitizers. Its universality is further exemplified by the seamless compatibility of a broad spectrum of alkyl halides and heteroarenes under standardized conditions, heralding a new era of synthetic versatility. The method's practicality is underscored by its capacity for late-stage modification of pharmaceuticals, offering a transformative tool for the enhancement of existing drug molecules. Moreover, the facile derivatization of the synthesized products underscores the method's adaptability and potential for diverse applications. Our mechanistic studies have elucidated the underlying radical-relay pathway, pinpointing the pivotal role of the EDA complex in initiating the transformation. This discovery not only enriches our fundamental understanding of the reaction but also opens avenues for strategic optimization.