Solid-Phase Synthesis of Diverse Macrocycles by Regiospecific\n2‑Pyridone Formation: Scope and Applications

This study introduces\na novel solid-phase macrocyclization method\ngenerating 2-pyridone rings. This method relies on the intramolecular\ncondensation between secondary and tertiary dimethoxy-propionic amide\nunits. This selective reaction leads to the formation of a single\nwell-defined regioisomer. The method demonstrates remarkable efficiency\nin producing diverse peptidic and nonpeptidic bioactive targets, paving\nthe way for the development of innovative macrocycle libraries featuring\nthe 2-pyridone unit.