Abstract
An efficient asymmetric synthesis of highly enantioenriched 3-hetero-substituted 2,3-dihydro-1 H-isoindolinones is reported. The key step is a diastereoselective nucleophilic addition on N-acylhydrazonium intermediates generated by acidic treatment of hemiaminal precursors bearing an ( S)-2-alkoxymethyl-pyrrolidin-1-yl type auxiliary. The auxiliary is removed by an oxidative N, N-bond cleavage with magnesium monoperoxyphthalate.
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