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Synthesis of Heterocycle-Bridged Peptidic Macrocycles through 1,3-Diyne Transformations.

  • December 1, 2016

Macrocyclic tetrapeptides containing a 1,3‐diyne tether are synthesized by using a mild Glaser–Hay‐type coupling and are subsequently treated with nucleophiles. This results in a variety of corresponding macrocycles bearing a heterocycle in the cyclic core structure. Boc = tert‐butoxycarbonyl.

 

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