Enantioselective Total Synthesis of (+)-Stephadiamine
An asymmetric synthesis of (+)-stephadiamine has been accomplished featuring (a) an enantioselective dearomatizative Michael addition to generate a quaternary stereocenter; (b) a domino sequence involving reductive generation of nitrone from γ-nitro ketone followed by a highly regio- and diastereo-selective intramolecular [3 + 2] cycloaddition to construct the aza[4,3,3]propellane core with concurrent generation of two quaternary stereocenters and two functional groups ready for subsequent transformations; (c) the Curtius rearrangement of the sensitive α,α-disubstituted malonic acid mono ester for the installation of α,α-disubstituted amino ester moiety; (d) a benzylic C–H oxidation under photoredox catalytic conditions; and (e) a highly diastereoselective ketone reduction affording δ-hydroxyester preorganized for lactonization.
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Yang, B., Li, G., Wang, Q., & Zhu, J. (2023). Enantioselective Total Synthesis of (+)-Stephadiamine. Journal of the American Chemical Society, 145(9), 5001–5006. https://doi.org/10.1021/jacs.3c00884
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2023-02-27
145
9
5001
5006
REVIEWED
EPFL