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One-Pot Solution-Phase Strategy for the Synthesis of Bicyclic Peptides Using the T3P/[Pd(PPh₃)₄] System

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Bicyclic peptides enhance receptor binding and proteolytic stability through conformational constraint, but their synthesis typically requires multistep assembly, orthogonal protection strategies, and repeated purification. This poster presents IRBM’s one-pot solution-phase route via bis-lactam cyclization, pairing head-to-tail macrolactamization with in situ Allyl/Alloc deprotection and spontaneous cross-link formation in a single vessel. A screen of coupling reagents and solvents reduces resin handling, reaction time, and solvent use while supporting reproducible scale-up. Download the poster to explore the reagent-solvent screen and cyclization workflow in detail.

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one-pot bis-lactam bicyclic peptides poster, code 26009

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