Process for the synthesis of a peptide having a trp residue

Process for the synthesis of a peptide having a trp residue

  • CN 101,003,563 A
  • Filed: 12/19/2001
  • Published: 07/25/2007
  • Est. Priority Date: 12/22/2000
  • Status: Active Application
First Claim
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1. a solid phase synthesis has the method for the peptide of general formula (II),A 1-A 2-A 3-Ser-A 5-A 6-Leu-A 8-Pro-A 10-R 1

  • (II)WhereinA 1Be Pyrrolidonecarboxylic acid or N-Ac-D-β


    A 2Be Histidine, D-p-Cl-Phe or D-p-F-Phe;

    A 3Be tryptophane, D-tryptophane, D-β

    -Nal or D-Pal;

    A 5Be tyrosine, NicLys, cPzACAla or PicLys;

    A 6Be D-β

    -Nal, D-hArg (Et) 2, D-Lys (iPr), D-hArg (Bu), D-hArg (CH 2CF 3) 2, D-His (Bzl), D-Leu, D-Pal, D-Ser (tBu), D-Trp, D-Cit, D-Arg, D-NicLys, D-PicLys or D-Qal;

    A 8Be arginine, hArg (Et) 2, hArg (Bu), hArg (CH 2CF 3) 2Or Lys (iPr);

    A 10Be glycine, NHNHCO or D-L-Ala or disappearance;

    With R 1Be NH 2Or NHEt;

    A wherein 3Or A 6In at least one is tryptophane or D-tryptophane;

    this method comprises the indoles-NH that uses provisional all tryptophan residues of protection of alkali labile side chain protected group, and wherein said blocking group is by being removed when solid support cutting has the peptide of general formula (II) with alkali reaction.

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