Abstract The synthesis of new and innovative macrocyclic amidinoureas from linear di-Boc- guanidino-alkylamines related to guazatine was accomplished. The macrocyclization reaction proceeds under mild conditions affording 11-to 16-membered rings with a new and previously undescribed structure in good yields. Enantiomerically pure macrocyclic amidinoureas were also synthesised. The strict correlation between macrocyclic ...