Diastereoselective Synthesis of N‐Heterocycle Substituted Cyclobutanes via Michael Addition onto Cyclobutenes

Abstract

Herein, we present a method for the diastereoselective synthesis of N‐heterocycle‐substituted cyclobutanes from commercially available bromocyclobutanes. This method enables the efficient formation of various heterocyclic aminocyclobutane esters and amides using simple reagents. Notably, N‐nucleophiles such as imidazoles, azoles, and nucleobase derivatives were successfully incorporated, enhancing the chemical diversity of small ring building blocks for medicinal chemistry applications.