A kind of preparation method of oxytocin

A kind of preparation method of oxytocin

CN
  • CN 106,589,069 B
  • Filed: 01/13/2017
  • Issued: 07/17/2018
  • Est. Priority Date: 01/13/2017
  • Status: Active Grant
First Claim
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1. a kind of preparation method of oxytocin, includes the following steps:

  • 1) using CTC resins as solid phase carrier, by amino acid protect monomer Boc-Cys (Trt)-OH, Fmoc-Tyr (tBu)-OH,Fmoc-Ile-OH, Fmoc-Gln (Trt)-OH, Fmoc-Asn (Trt)-OH, Fmoc-Cys (Trt)-OH are in condensing agent and alkalinityUnder the conditions of carry out condensation reaction successively, from resin cut after obtain the first intermediate;

    The condensation reaction is with reagent of raising one'"'"'s hatPiperazine,The amino acid sequence of first intermediate is:

    Boc-Cys(Trt)-Tyr(tBu)-Ile-Gln(Trt)-Asn(Trt)-Cys(Trt)-OH;

    2) using Fmoc-Pro-Leu-OH, Gly-NH2, BOP and HOBt as raw material, Fmoc-Pro-Leu-Gly-NH2 is synthesized, with twoEthamine sloughs the Fmoc in the Fmoc-Pro-Leu-Gly-NH2, obtains the second intermediate;

    The amino of second intermediateAcid sequence is:

    H-Pro-Leu-Gly-NH2;

    3) the first intermediate that the step

         1) obtains and the second intermediate that step

         2) obtains are subjected to condensation reaction, it is usedCondensing agent is DCC-HOOBt or DPPA or DCC-HOBt, obtains oxytocin precursor 1, the amino acid sequence of the oxytocin precursorFor:

    Boc-Cys(Trt)-Tyr(tBu)-Ile-Gln(Trt)-Asn(Trt)-Cys(Trt)-Pro-Leu-Gly-NH2;

    4) Trt in the oxytocin precursor 1 that the step

         3) obtains is sloughed with iodine, forms disulfide bond, then had after cutting peptideThere is the oxytocin of structure shown in Formulas I;

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