TiF-catalyzed direct amidation of carboxylic acids and amino acids with amines.

Org Biomol Chem

Department of Chemistry, Purdue University, West Lafayette, Indiana 47907, USA.

Published: February 2024

Unlike other metal fluorides, catalytic titanium tetrafluoride enhances the direct amidation of aromatic and aliphatic carboxylic acids and -protected amino acids in refluxing toluene. While aromatic acids were converted to amides with 10 mol% of the catalyst within 24 h, aliphatic acids underwent a faster reaction (12 h), with lower catalyst loading (5 mol%). This protocol is equally efficient with alkyl and aryl amines providing a variety of carboxamides and peptides in 60-99% yields.

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http://dx.doi.org/10.1039/d3ob01943hDOI Listing

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