Conformationally stable peptide macrocycles assembled using the Petasis borono-Mannich reaction.

Akitake Yamaguchi,Sherif J Kaldas,Solomon D Appavoo,Diego B Diaz,Andrei K Yudin

CHEMICAL COMMUNICATIONS（2019）

Cited 12|Views3

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Abstract

Macrocyclization of linear peptide precursors using the Petasis borono-Mannich reaction affords a diverse range of macrocycles with an endocyclic amine. Analysis of the corresponding macrocyclic structures underscores that the hydrogen bond between an endocyclic amine and the adjacent amide NH is a powerful control element for conformationally homogenous peptide macrocycles.

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Key words

Peptide Synthesis,Solid-Phase Synthesis

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