Mohy El Dine, Tharwat Erb, William Berhault, Yohann Rouden, Jacques Blanchet, Jérôme Catalytic Chemical Amide Synthesis at Room Temperature: One More Step Toward Peptide Synthesis An efficient method has been developed for direct amide bond synthesis between carboxylic acids and amines via (2-(thiophen-2-ylmethyl)­phenyl)­boronic acid as a highly active bench-stable catalyst. This catalyst was found to be very effective at room temperature for a large range of substrates with slightly higher temperatures required for challenging ones. This methodology can be applied to aliphatic, α-hydroxyl, aromatic, and heteroaromatic acids as well as primary, secondary, heterocyclic, and even functionalized amines. Notably, <i>N</i>-Boc-protected amino acids were successfully coupled in good yields with very little racemization. An example of catalytic dipeptide synthesis is reported. functionalized amines;carboxylic acids;heteroaromatic acids;Catalytic Chemical Amide Synthesis;Room Temperature;room temperature;catalyst;dipeptide synthesis;amide bond synthesis;Peptide SynthesisAn 2015-05-01
    https://acs.figshare.com/articles/journal_contribution/Catalytic_Chemical_Amide_Synthesis_at_Room_Temperature_One_More_Step_Toward_Peptide_Synthesis/2170669
10.1021/acs.joc.5b00378.s001