Palladium-Catalyzed cross-Benzannulation of Aminoenynes with Diynes. Highly Regioselective Synthesis of Polysubstituted Anilines.

Polysubstituted anilines were prepared by the palladium-catalyzed cross-benzannulation of conjugated aminoenynes 1-4 with diynes 8. The reaction proceeded in a highly regioselective manner under mild conditions, and the anilines were obtained as single regioisomers. Our method complements the well-known precedures for the preparation of polysubstituted anilines which are widely used in organic synthesis.