Palladium‐Catalyzed Preparation of N‐Alkylated Tacrine and Huprine Compounds

Abstract An efficient preparation of N ‐alkylated tacrine and huprine compounds using palladium‐catalyzed amination was developed. Cross‐coupling reactions with chloroquinolines and primary amines were achieved in good to excellent yields (50–95 %) following microwave irradiation. This method was found particularly useful for functionalized substrates which undergo degradation under S N Ar conditions and for the synthesis of tacrine‐ and huprine‐based heterodimeric inhibitors, examples of which are described.