Highly Reactive,General,and Long-Lived Catalysts for Coupling Heteroaryl and Aryl Chlorides with Primary Nitrogen Nucleophiles

摘要

During the past decade,the palladium-catalyzed amination of aryl halides has become a principal method to form the C-N bonds of aromatic amines.Although current catalysts are capable of coupling a wide range of amines with aryl halides,reactions with these catalysts have several limitations: the catalysts have short lifetimes in the reactions of primary amines with chloroarenes,even when conducted with the most recently developed,highly active catalysts containing basic,hindered alkylmonophosphines;the reactions of primary alkyl amines with heteroaryl chloride reagents,which are important for the synthesis of biologically active molecules,have limited scope and require large amounts of catalyst;and the reactions of primary alkyl amines with chloroarenes that possess common protic functional groups have not been described.