Abstract
Cyclobutenes serve as valuable scaffolds in pharmaceutical development, but synthesizing structurally diverse fully C-substituted cyclobutenes remains challenging. Here we report a stereoselective [2 + 2] cycloaddition between alkynyl 1,3-dithianes and cinnamate esters using a catalytic amount of KOtBu. Our approach enables the construction of synthetically challenging tetrasubstituted cyclobutenes via anion relay chemistry (ARC), exhibiting excellent trans-diastereoselectivities (dr > 20:1).
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