This article draws on the work of Li et al. on the TCFH/catalytic Oxyma system and transient imine protection, and summarizes design strategies for the selective acylation of less reactive amines in complex substrates. The discussion below focuses on identifying competing reactive sites, ...
TFPN [tetrafluorophthalonitrile, 3,4,5,6-tetrafluorophthalonitrile] has in recent years been used for amide bond and peptide bond formation under carboxylic acid activation conditions. Published studies have shown that this route can be applied to sterically hindered substrates and difficult ...
In peptide synthesis, what is often truly difficult to control is not whether an amide bond can be formed, but rather how to minimize epimerization at the α-stereogenic center of the activated carboxylic acid component during activation and the subsequent bond-forming process. This issue is ...
“Racemization” in peptide synthesis is often discussed as if it were mainly a question of whether one coupling reagent is better than another. From the standpoint of reaction chemistry, however, what deserves greater caution is the period after the carboxylic acid has been activated. In many ...
TBTU [O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate] has long been one of the most commonly used coupling reagents for carboxylic acid activation and amide bond formation, and has been widely employed in both solution-phase amidation and solid-phase peptide synthesis ...
The most familiar route from nitro compounds to amides is usually to first reduce the nitro group to an amine, and then react that amine with a carboxylic acid derivative or an activated carboxylic acid system. This route is mature, reliable, and remains the most common choice in both laboratory ...
Amide bond formation is one of the most common fundamental reactions in organic synthesis, medicinal chemistry, and peptide chemistry. For a long time, when evaluating coupling reagents, the first concerns were usually whether the reaction was fast enough, whether the yield was high enough, and ...
Amide bond formation is one of the most common fundamental transformations in the synthesis of drug molecules, natural products, and functional molecules. In efforts to improve amidation reactions, researchers are concerned not only with whether a bond can be formed, but also with whether the ...
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