Toward mechanized peptide synthesis via polymeric reagents approach

Simultaneous application of high-molecular-weight active esters and polyvinylN,N- diethylbenzylamine was used as a basis for a continuous peptide synthesis via the polymeric reagents approach. Using the synthetic procedure developed, the hexapeptide Boc-L-Pro-L-Val-L-LysZ(p-NO₂)]-L-Val-L-Tyr(Dnp)-L-Pro-OBzr¹ and the tetrapeptide Boc-l-LysZ(p-NO₂)]-L-LysZ(p-NO₂)]-L-Arg(NO₂)-L-Arg(NO₂)-OBzr, corresponding to residues 19–24 and 15–18 of human ACTH, were synthesized in 63 and 70% overall yields, respectively.