A practical, one‐pot protocol is described for the conversion of carboxylic acids into amides through carboxyl activation by the reagent combination of trimethyl phosphite and iodine. This method integrates several advantages: (1) it allows amines to be chemoselectively acylated with excellent results in the presence of sulfur and oxygen nucleophiles; (2) the method shows wide generality in respect of solvent, base, and substrate; (3) the reagents used are widely available and much less expensive than common coupling reagents, and (4) the process is remarkably convenient, permitting extraction, recrystallization, and column chromatography as optional work‐up procedures. The chemoselectivity and generality of the method, the low cost, and wide availability of reagents combined with the ease of use make it a very favorable process.

the direct N-acylation of amines with carboxylic acids is presented to afford a wide variety of aromatic and aliphatic amides. A diversity of functional groups is tolerated, including ester, ether, aromatic halides and double bonds. This method can also be extended to peptide synthesis [cf. (XV)]. The reaction involves activation of the carboxylic acid with in situ generated dimethyl iodophosphate in the presence of base. Interestingly, excellent chemoselectivity for N-acylation is observed in the presence of alcohols or thiols. -(LUO*, Q.-L.; LV, L.; LI, Y.; TAN, J.-P.; NAN, W.; HUI, Q.; Eur. J. Org. Chem. 2011, 34, 6916-6922, http://dx.doi.org/10.1002/ejoc.201101030 ; Coll. Chem. Chem. Eng., Southwest Univ., Chongqing, Sichuan 400715, Peop. Rep. China; Eng.) -Mischke 18-043