Flow Electroreductive Nickel‐Catalyzed Cyclopropanation of Alkenes Using <i>gem</i>‐Dichloroalkanes

Morgan Regnier, Clara Vega, Dimitris I. Ioannou, Zhenyu Zhang

Angewandte Chemie International Edition · 2025 · 17 citations · 63 references

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Abstract

Cyclopropanes are valuable motifs in organic synthesis, widely featured in pharmaceuticals and functional materials. Herein, we report an efficient electrochemical methodology for the cyclopropanation of alkenes, leveraging a nickel-catalyzed process in continuous-flow. The developed protocol demonstrates broad substrate scope, accommodating both electron-rich and electron-poor alkenes with high functional group tolerance. Beyond dichloromethane as a feedstock methylene source, the methodology enables the synthesis of methylated, deuterated, and chloro-substituted cyclopropanes. Mechanistic investigations suggest the electro-generation of a nickel carbene as key intermediate. Notably, the reaction operates under ambient conditions, tolerates air and moisture, and achieves scalability through continuous-flow technology, offering a straightforward route to multi-gram quantities with enhanced throughput.

References

63