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The diastereoselective Mannich reaction of functionalized aldehydes, using a phenethylamine‐derived iminium precursor, by activation with prolines and prolinol derivatives have been studied. Optimized reaction conditions have been developed, allowing for scale‐up and preparation of γ‐amino alcohol derivatives on multi‐gram scale from β‐hydroxypropanal and ‐butanal, with diastereoselectivites of typically...
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