High Efficiency Synthesis of Phosphopeptides

Introduction

Highly efficient synthesis of difficult phosphopeptides is demonstrated using the Liberty BlueTM automated microwave peptide synthesizer with CarboMAXTM 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).