Regio- and Diastereoselective Aminopyridylation of Bicyclo[1.1.0]butanes with N‑Aminopyridinium Ylides Enabled by Photoredox Catalysis

Visible-light-mediated functionalization of bicyclo[1.1.0]butanes (BCBs) has been proven to be an efficient way to obtain diverse cyclobutane derivatives. However, achieving diastereoselective control in this field remains challenging. Herein, we reported a mild photoredox-catalyzed aminopyridylation of BCBs with N-aminopyridinium ylides, delivering the cyclobutylamine derivatives with excellent regio- and diastereoselectivities. This protocol demonstrated excellent compatibility with a wide range of BCBs and N-aminopyridinium ylides, and the value of this approach was highlighted by its application in the preparation of high-value, structurally complex cyclobutane derivatives.