Abstract

The first synthesis of rigid pentacyclic NORPHOS derivatives by a tandem cross-coupling/cross-dehydrogenative-coupling according to the Catellani reaction protocol is reported. Mediated by palladium complexes of C,P-chelating monophosphine ligands, the readily available enantiopure NORPHOS oxide underwent a stereo- and regio-selective cyclocondensation reaction with arylhalides involving the activation of two unreactive C–H bonds.

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