Ligand-Promoted C3-Selective Arylation of Pyridines with Pd Catalysts: Gram-Scale Synthesis of (±)-Preclamol

摘要

The first example of Pd-catalyzed, C3-selec-tive arylation of unprotected pyridines has been developed by employing a catalytic system consisting of Pd(OAc)_2 and 1,10-phenanthroline. This protocol provides an expeditious route to an important class of 3-arylpyridines and 3-arylpi-peridines frequently found in bioactive compounds. A brief synthesis of the drug molecule (±)-predamol is also reported.