Cyclic depsipeptides, bioactive natural products containing ester(s) and amides in the macrocycle, are synthesized via 3 strategies, macrolactamization in solution, macrolactamization on-resin, and macrolactonization.
This review focuses on recent developments in solid- and solution-phase continuous-flow peptide synthesis over the past four years.
Tissue transglutaminase (TG2) is both an enzyme and a G-protein that is implicated in many diseases, such that small molecule inhibitors of TG2 have broad potential as drugs or research tools.
Amine bases go beyond their typical proton shuttle role in the macrolactamization of pseudoxylallemycin, as we diastereoselectively synthesize the natural product and analogues thereof to explore their characterization and biological activity.
We report a chemoselective amide coupling strategy that selectively reacts with hindered amine in the presence of competing primary alcohols and amines with excellent chemoselectivity, reactivity, and minimal epimerization.