Application of an automated synthesis suite to parallel solution-phase peptide synthesis

An in-house developed automated synthesis suite was used to prepare a libra ry of 72 tetrapeptide derivatives, the starting materials for pharmaceutica lly attractive pentapeptides, employing a convergent strategy. An initial s et of 18 dipeptides were synthesized on a large-scale (100-1000g) using aut omated synthesis workstations, and then 72 tetrapeptides were synthesized o n a medium scale (5-10 g) using an automated system. Each di- or tetrapepti de was prepared in a single operating cycle using a modified methanesulfoni c acid method, then a sub-library of 56 pentapeptides were synthesized in p arallel, on a small-scale (100 mg-1 g) using a robotic workstation.