Multicomponent Functionalization of the Octreotide Peptide Macrocyclic Scaffold,European Journal of Organic Chemistry

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Multicomponent Functionalization of the Octreotide Peptide Macrocyclic Scaffold
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2022-08-01 , DOI: 10.1002/ejoc.202200687
Aldrin V. Vasco ₁ , Leonardo G. Ceballos ₂ , Ludger A. Wessjohann ₁ , Daniel García Rivera ₃

Affiliation

New octreotide analogs were prepared by replacing the disulfide bond with a functionalized tertiary lactam bridge. The on-resin approach includes an Ugi multicomponent macrocyclization that enables the simultaneous ring closure and incorporation of lipids, fluorophores and functional groups suitable for the subsequent conjugation to cytotoxic moieties.

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