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  • Title: Palladium(0)-catalyzed regioselective and multicomponent synthesis of 1,2,3-trisubstituted 1H-indenes.
    Author: Tsukamoto H, Ueno T, Kondo Y.
    Journal: Org Lett; 2007 Aug 02; 9(16):3033-6. PubMed ID: 17616142.
    Abstract:
    A multicomponent synthesis of biologically important indenes bearing three substituent groups at the 1-, 2-, and 3-positions from available o-ethynylbenzaldehyde derivatives and organoboron reagents under palladium(0) catalysis is described. A two-component coupling reaction in methanol provides 1H-indenols, whereas a three-component reaction involving secondary aliphatic amines as the third component in DMF affords 1H-indenamines. This method allows combinatorial preparation of unsymmetrically substituted 1H-indenes that cannot be prepared via previous synthetic routes.
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