Modular Synthesis of Multi‐substituted Cyclobutanones Enabled by Oxyallyl Cations†

Abstract

Comprehensive SummaryStereoselective synthesis of multi‐substituted cyclobutanes with different substituents is still a daunting challenge in organic synthesis. We report here a practical and facile approach to synthesizing all‐trans 2,3,4‐trisubstituted cyclobutanones from readily available dichlorocyclobutanones. The substitution reaction proceeds smoothly via oxyallyl cation intermediates under mild basic conditions. Further transformation to the synthesis of 1,2,3,4‐tetrasubstituted cyclobutanes was also explored.