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Enantioselective Organocatalytic Intramolecular Aza‐Diels–Alder Reaction
Abstract:A highly efficient catalytic enantioselective intramolecular Povarov reaction was developed with primary anilines as 2‐azadiene precursors. A wide variety of angularly fused azacycles were obtained without column chromatography in high to excellent yields and with excellent diastereo‐ and enantioselectivity (d.r.>99:1 and up to e.r. 99:1). Furthermore, the catalyst loading could be lowered to 1 mol %, and the obtained azacycles could be used as key intermediates for further transformations to generate additional molecular diversity.
Keywords:Chirale Phosphorsä  uren  Cycloadditionen  Heterocyclen  Intramolekulare Povarov-Reaktion  Wasserstoffbrü  cken
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