期刊
TETRAHEDRON
卷 63, 期 36, 页码 8855-8871出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2007.06.019
关键词
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Polystyrene-IIDQ, a polymer-supported coupling reagent, was synthesized in three steps from Merrifield resin in 86% overall conversion. This reagent efficiently coupled carboxylic acids to amines in good yields and high purities, required no pre-activation step, and was tolerant of the order of reagent addition. PS-IIDQ was observed to be more efficient than polymer-supported carbodiimides (PS-EDC and PS-DCC) and gave higher yields than HATU for general amide bond formation, including the coupling of anilines and hindered substrates. When evaluated with five carboxylic acids and nine amines (including anilines and secondary amines) PS-IIDQ gave an average isolated yield of 73%. (c) 2007 Elsevier Ltd. All rights reserved.
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