A kind of method of improved Fmoc Solid-phase synthesis peptides oxytocin

A kind of method of improved Fmoc Solid-phase synthesis peptides oxytocin

CN
  • CN 106,243,194 B
  • Filed: 09/12/2016
  • Issued: 08/17/2018
  • Est. Priority Date: 09/12/2016
  • Status: Active Grant
First Claim
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1. a kind of method of improved Fmoc Solid-phase synthesis peptides oxytocin, it is characterised in that:

  • Include the following steps:

    1) using Rink Amide AM resins as solid phase carrier, using Fmoc protected amino acids as monomer, N-terminal Boc-Cys(Acm)-OH, piperazine solution are reagent of raising one'"'"'s hat, and under condensing agent and alkaline condition effect, connect amino acid one by one successively, synthesizeOxytocin;

    2) it sloughs Acm with iodine while forming disulfide bond on solid phase carrier, obtain cyclisation protection oxytocin sequence;

    3) it carries out cutting peptide, concentrates, obtain the crude product of oxytocin;

    4) after purifying crude product, oxytocin product is obtained;

    In step

         1), the Replacement rate of the Rink Amide AM resins is 0.55mmol/g;

    The amino acid monomer of protection is:

    Fmoc-Gly-OH、

    Fmoc-Leu-OH、

    Fmoc-Pro-OH、

    Fmoc-Cys(Acm)-OH、

    Fmoc-Asn(Trt)-OH、

    Fmoc-Ile-OH, Fmoc-Gln (Trt)-OH, Fmoc-Tyr (tBu)-OH and Boc-Cys (Acm)-OH, the rate of charge of amino acid monomerFor 2 equivalents of degree of substitution;

    The solvent of the piperazine solution is DMF, a concentration of 0.1~1mol/L of piperazine solution;

    The condensationAgent is HBTU, and condensing agent rate of charge is the 0.95-1 equivalents of amino acid;

    The alkali be DIEA, alkali rate of charge amino acid 1~1.5 equivalent;

    The oxytocin amino acid sequence is

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