Abstract The synthesis of a variety of potent macrocyclic growth hormone secretagogues, ie 5, 9, 12, and 20–22, based on the known lead structure L-692,429 (1) is described. These conformationally constrained growth hormone secretagogues were prepared by joining the two essential pharmacophores, the amino-acid side chain at the 1H-1-benzazepine moiety and the 1, 1′-biphenyl moiety with a variety of linkers. The most potent analog was found ...
