Application of an automated synthesis suite to parallel solution-phase peptide synthesis.
An in-house developed automated synthesis suite was used to prepare a library of 72 tetrapeptide derivatives, the starting materials for pharmaceutically attractive pentapeptides, employing a convergent strategy. An initial set of 18 dipeptides were synthesized on a large-scale (100-1000 g) using automated synthesis workstations, and then 72 tetrapeptides were synthesized on a medium scale (5-10 g) using an automated system. Each di- or tetrapeptide was prepared in a single operating cycle using a modified methanesulfonic acid method, then a sub-library of 56 pentapeptides were synthesized in parallel, on a small-scale (100 mg-1 g) using a robotic workstation.
Kuroda
N
N
Discovery Research Division, Takeda Chemical Industries, Ltd., Osaka, Japan. Kuroda_Noritaka@takeda.co.jp
Hattori
T
T
Fujioka
Y
Y
Cork
D G
DG
Kitada
C
C
Sugawara
T
T
D002264:Carboxylic Acids / Q000138:chemical synthesis; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004151:Dipeptides / Q000138:chemical synthesis; D004952:Esters / Q000138:chemical synthesis; D009842:Oligopeptides / Q000138:chemical synthesis*; D019151:Peptide Library; D011786:Quality Control; D012996:Solutions; D013237:Stereoisomerism
D002264:Carboxylic Acids; D004151:Dipeptides; D004952:Esters; D009842:Oligopeptides; D019151:Peptide Library; D012996:Solutions