![EurJOC](/sites/default/files/styles/original_ratio_zero/public/2021-07/16c094f04e.png?itok=AxpxF2rV)
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.