Acetonitrile Activation: An Effective C2 Cyclization Unit

A novel acetonitrile activation for construction of cyclobutenones via [2+2] cyclization is developed. Acetonitrile is utilized for the first time as C2 cyclization building block. The present protocol successfully inhibits the competitive cycloaddition with the C≡N triple bond, but enables the in situ formation of unsaturated carbon‐carbon bond and the subsequent cycloaddition as a C2 unit. This chemistry features simple reaction conditions, high chemoselectivities, wide substrate scopes, and offers a new and practical approach to cyclobutenones and cyclobuteneimines.

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