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Improved Gram-Scale Procedure for MIBA-Catalyzed Direct Amidation and Its Application to the Preparation of alpha and beta PeptidesDownload
Direct condensation between a carboxylic acid and amine must overcome the initial formation of a thermodynamically stable and unreactive carboxylate-ammonium salt, providing the amide product only at very high temperatures (over 160 oC) that are incompatible with many functionalized molecules....
The development of rapid and bioorthogonal chemical reactions has expanded greatly the utility of bioconjugation chemistry in the service of site-selective protein labeling, even allowing molecular imaging in live cells or animals. âClickâ chemistry is particularly desirable due to its fast...