Synthesis of Indolines by a Zn-Mediated Mannich Reaction/Pd-Catalyzed Amination Sequence
Marc Presset, Antoine Pignon, Jérôme Paul, Erwan Le Gall* , Eric Léonel and Thierry Martens
*Électrochimie et Synthèse Organique, Université Paris Est, ICMPE (UMR 7182), CNRS, UPEC, 2-8 rue Henri Dunant, F-94320 Thiais, France, Email: legallicmpe.cnrs.fr
M. Presset, A. Pignon, J. Paul, E. Le Gall, E. Léonel, T. Martens, J. Org. Chem., 2017, 82, 3302-3310.
DOI: 10.1021/acs.joc.7b00013 (free Supporting Information)
see article for more reactions
1,2-Disubstituted indolines have been prepared in good yields by a Zn-mediated organometallic Mannich reaction, followed by an intramolecular Buchwald-Hartwig reaction. The reactions are easy to set up and compatible with a broad range of simple or commercially available reagents. The method was further extended to the preparation of a 1,2,3-trisubstituted indolines.
see article for more examples