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摘要
The Sonogashira coupling reaction of polymer-supported propargylamine (= prop-2-yn-1-amine) with aryl iodides in the presence of the [Pd(PPh(3))(2)]Cl(2)/Cul catalyst system produces 3-arylprop-l-yn-1-amines smoothly at room temperature (Scheme). When propargylamine is attached on Wang resin through a carbamate linker, the common problems with amino functionality in palladium-catalyzed couplings are overcome. The arylpropynamines are cleaved from the polymer with CF(3)COOH and converted into chromatographically easily separable acetamides. Our solid-phase method opens a new pathway toward precursors of pharmacologically interesting arylpropynamines and arylpropanamines.
- 出版日期2010
