Synthesis of CF3-containing α-alkynyl-α-aminophosphonates by Sonogashira cross-coupling reaction

An efficient route to new alpha-CF3-alpha-aminophosphonic acid derivatives bearing an arylalkynyl moiety at the alpha-carbon atom has been developed. The method is based on palladium-catalyzed cross-coupling of the corresponding alpha-propargyl (ethynyl) alpha-aminophosphonates with aryl iodides to afford the aminophosphonic acid derivatives with an internal triple bond that is suitable for further modifications. (C) 2011 Elsevier B.V. All rights reserved.