Demonstrates a metal-free method to synthesize BCPs from [1.1.1]propellane, suggesting a simpler approach to drug discovery.
Aryl-substituted bicyclo[1.1.1]pentanes (BCPs) are valuable scaffolds in drug discovery. However, their synthesis typically requires multistep sequences via prefunctionalized [1.1.1]pentane. Herein, we report a metal-free, visible-light-driven three-component dicarbofunctionalization of [1.1.1]propellane via an electron donor-acceptor (EDA) complex. This method provides direct and diverse access to 1,3-disubstituted BCPs under mild conditions with operational simplicity and green chemistry, featuring good functional group tolerance from readily available starting materials.
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Huo et al. (2026) studied this question.
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