Ideas Behind the Tryptophan‐Mediated Petasis Reaction (TMPR) Concept for Peptide Stapling

Abstract

This Concept short review offers an insightful analysis of pivotal research papers and explores the key synthetic ideas behind the intersection of two realms in peptide chemistry: using tryptophan and Petasis multicomponent reactions for macrocyclisation and labelling of peptides. The recently published tryptophan‐mediated Petasis reaction (TMPR) concept represents a critical junction between these two worlds, highlighting how combining such methodologies leads to more effective and versatile synthetic strategies, setting a potentially new direction for future research in the field of peptide‐drug conjugates.