Synthetic polystyrene resin and its use in solid phase peptide synthesis

Claim 1

A process for the manufacture of peptides or peptide amides, characterised in that (a) a synthetic resin based on polystyrene which is crosslinked with from 0 to 5 mol % of divinyl benzene and wherein benzene rings of the skeletal structure are substituted by groups of the formula ##STR6## in which X represents --O-- or --NH-- and R represents C 1 -C 4 -alkyl is reacted with a compound of formula W 1 --AM 1 --Y--H, in which Y represents --O-- or --NH--, W 1 represents an N-terminal amino-protecting group and AM 1 represents the acyl radical of an amino acid sequence, consisting of from 1 of 25 amino acid residues, in which functional groups are protected or unprotected, or with a reactive functional derivative thereof, for the purpose of attaching the W 1 --AM 1 --residue to the --X-- group of the resin, (b) the N-terminal protecting group W 1 is removed, (c) the freed N-terminal amino group is acylated by reaction with an acid of formula W 2 --AM 2 --OH, in which W 2 represents an N-terminal amino protecting group and AM 2 represents the acyl radical of an amino acid sequence, consisting of from 1 to 25 amino acid residues, in which functional groups are protected or unprotected, or with a reactive functional derivative thereof, (d) the operation of alternate removal according to (b) and acylation according to (c) is repeated as required until the desired amino acid sequence is obtained, and (e) the resulting peptide or peptide amide, prior to, after, or with simultaneous removal of any protecting group, is detached from the resin by acidolysis with a mild acidic agent selected from the group consisting of trifluoroacetic acid, a lower alkanecarboxylic acid, a pyridinium salt, and mixtures thereof with an inert organic diluent.