A New Approach to Substituted Cyclobutanes: Direct β-Deprotonation/ Magnesiation of Cyclobutane Carboxamides

Abstract
BuMgN(i-Pr)2 is shown to be kinetically and thermodynamically efficient for deprotonation/magnesiation cis and β to an activating carboxamido group on a cyclobutane ring. The resulting carboxamido-stabilized amido-Grignards are useful reagents. The method provides an entirely new approach to controlled substitution on cyclobutanes. BuMgN(i-Pr)2 will also metalate pivaloyl amides.

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