Method for synthesizing atosiban acetate from solid phase polypeptide

A solid-phase peptide synthesis, atosi-like technology, applied in the preparation methods of peptides, chemical instruments and methods, peptides, etc., can solve the problems of complex operation, high labor cost, and three wastes.

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A solid-phase peptide synthesis, atosi-like technology, applied in the preparation methods of peptides, chemical instruments and methods, peptides, etc., can solve the problems of complex operation, high labor cost, and three wastes.

CN101357937AActive Publication Date: 2009-02-04SHANGHAI SOHO YIMING PHARMA

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Embodiment 1

[0160] Peptide chain preparation:

[0161] Weigh the amount of Rink Amide AM resin equivalent to 720mmol (200 mesh, 0.80mmol / g), put it into the SHYM-25 peptide synthesizer, soak it in 6000ml DMF to swell the resin, and drain it. Add 6400 ml of a DMF solution with a volume concentration of 25% hexahydropyridine, and shake at 25° C. for 30 minutes. Drain, wash several times with DMF, respectively, and drain.

[0162] Preparation of Fmoc-Gly-resin:

[0163] Add Fmoc-Gly-OH (MW: 297.3, 1440mmol) 428g, HOBT (MW: 135.1, 1440mmol) 195g, TBTU (MW: 321, 1440mmol) 462g, NMM 320ml (MW = 101.2), 4000ml DMF, shake the mixture at 25°C Shake for 1.5 hours. Drain, wash with DMF several times, and drain.

[0164] Preparation of Fmoc-Orn(Boc)-Gly-resin:

[0165] Add 6400 ml of a DMF solution with a volume concentration of 25% hexahydropyridine, and shake at 25° C. for 30 minutes. Drain, wash several times with DMF, and drain.

[0166] Fmoc-Orn (Boc)-OH (MW: 454.5, 1440mmol) 654g, TBTU (...

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Abstract

The invention discloses a preparation method of solid phase peptide synthesis atosiban which includes the following steps: taking Rink Amide resins, Rink Amide MBHA resins or Rink Amide AM resins as starting materials and taking Fmoc amino acids as monomers, amino acids are grafted one by one and mercaptopropionic acids (Map(SX)) are protected by the last peptide chain; after protected nonapeptide resins are obtained, the acellular side-chain protective groups and cutting peptides are synchronized; then cutting peptides is carried out, and reduced crude atosiban is collected; the pH value is adjusted to 7.5 to 10.0, and oxidized crude atosiban is collected; target products are obtained by the separation and purification by preparative HPLC(C18 or C8 column). The preparation method is convenient in material source, simplifies technology and reduces cost; and the preparation method is low in the pollution of three wastes and is high in yield, and the preparation method is convenient for being industrialized and has good industrialization prospect.

Description

technical field [0001] The invention relates to a preparation method of atosi-like, in particular to a preparation method of solid-phase polypeptide synthesis of atosi-like. Background technique [0002] Chinese name: Atosiban, Atosiban acetate, Atosiban, Atosiban acetate. [0003] English name: Atosiban, Atosiban Acetate. [0004] The structural formula is: [0005] [0006] The molecular formula is: C 43 h 67 N 11 o 12 S 2 [0007] Molecular weight: 994.2 [0008] Atosi is generally clinically a cyclic peptide oxytocin competitive antagonist that can be injected intravenously on receptors in the uterus, decidua, and fetal membranes. After using this product, it can inhibit uterine contractions in a dose-related manner, and reduce the secretion of prostaglandins mediated by the cyclic peptide oxytocin, so as to achieve the purpose of fetal protection. It can be used for people over 18 years old, with a gestational age of 24-33 weeks, and a normal fetal heart rat...

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Application Information

Patent Timeline

04 Feb 2009

Publication

CN101357937A

IPC: C07K7/06; C07K1/04

CPC: Y02P20/55

Inventors: 崔颀; 周逸明