High Efficiency Synthesis of Phosphopeptides

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Highly efficient synthesis of difficult phosphopeptides is demonstrated using the Liberty Blue™ automated microwave peptide synthesizer with CarboMAX™ coupling methodology. The use of microwave energy proved powerful for coupling bulky phosphoamino acid derivatives while the use of CarboMAX coupling methodology stabilized the acid-labile protected phosphate group at high temperature thereby minimizing side reactions. Using this approach the following phosphopeptides were each assembled in less than 2 hours: CTEDQY(pS) LVED-NH2 (82% purity), CPSPA(pT)DPSLY-NH2 (73% purity), and CSDGG(pY)MDMSK-NH2 (62% purity).