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 SNAr conditions and for the synthesis of tacrine- and huprine-based heterodimeric inhibitors, examples of which are described.
Palladium-Catalyzed Preparation of N-Alkylated Tacrine and Huprine Compounds
Ronco C;
2011
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 SNAr conditions and for the synthesis of tacrine- and huprine-based heterodimeric inhibitors, examples of which are described.File in questo prodotto:
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