biostudies-literatureProcter RJInstitució Catalana de Recerca i Estudis AvançatsEngineering and Physical Sciences Research Council4718-4724https://www.ebi.ac.uk/biostudies/studies/S-EPMC11831689biostudies-literatureUnknown16(11)The catalytic activity of different classes of boron catalysts was studied in amidation reactions with 4-phenylbutylamine/benzoic acid, and with 2-aminopyridine/phenylacetic acid. Whilst a simple boronic acid catalyst showed high catalytic activity with the former substrates, it was completely inactive in the latter reaction. In contrast, a borate ester catalyst was able to mediate the amidation of both substrate pairs with moderate activity. By screening a range of borate esters we were able to identify a novel borate catalyst that shows high reactivity with a range of challenging carboxylic acids/amine pairs, enabling catalystic amidation reactions to be achieved effectively with these industrially relevant compounds. The reactions can be performed on multigram scale with high levels of Chemical scienceBorate-catalysed direct amidation reactions of coordinating substrates.PMC11831689EP/T030534/1EP/T030666/1EP/T030658/1EP/T030488/1Procter RJDumon ASWhiting AAlamillo-Ferrer CShabbir URzepa HSBucar DKBritton PSheppard TDBures JfalseBorate-catalysed direct amidation reactions of coordinating substrates.The catalytic activity of different classes of boron catalysts was studied in amidation reactions with 4-phenylbutylamine/benzoic acid, and with 2-aminopyridine/phenylacetic acid. Whilst a simple boronic acid catalyst showed high catalytic activity with the former substrates, it was completely inactive in the latter reaction. In contrast, a borate ester catalyst was able to mediate the amidation of both substrate pairs with moderate activity. By screening a range of borate esters we were able to identify a novel borate catalyst that shows high reactivity with a range of challenging carboxylic acids/amine pairs, enabling catalystic amidation reactions to be achieved effectively with these industrially relevant compounds. The reactions can be performed on multigram scale with high levels of 2025-01-01T00:00:00Z2025 Mar2026-05-29T15:22:04.716Z2025-04-04T02:12:43.084ZS-EPMC118316893996828610.1039/d4sc07744j