IMPROVED SOLID-PHASE PEPTIDE SYNTHESIS AND AGENT FOR USE IN SUCH SYNTHESIS

摘要

Peptides X-AA1-AA2...AA n-Y, wherein AA is an L- or D-amino acid residue, X ishydrogen or an amino protective group, Y is OH,NH2 or an amino acid sequence comprising from 3 to 9 amino acid residues and nis an integer greater than 2, are prepared by solid phasesynthesis, preferably using Fmoc-chemistry, the improvement consisting in thatthe C-terminal part attached to the solid phase comprises apre-sequence comprising from 3 to 9, preferably from 5 to 7, amino acidresidues independently selected from native L-amino acids havinga side chain functionality which is suitably protected during the couplingsteps and having a propensity factor P.alpha. 0.57 and a propensityfactor P.beta. 1.10, preferably Lys and/or Glu, or the corresponding D-aminoacids and said pre-sequence is optionally cleaved from theformed peptide.