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Synthetic method of carbetocin acetate

A technology of carbetocin and synthesis method, which is applied in the field of carbetocin synthesis, can solve the problems of unsuitability for actual production and complicated operation, and achieve the effects of less reaction steps, cheap reagents, and less environmental pollution

Pending Publication Date: 2020-06-02
XIANGYU PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This method is complicated to operate and is not suitable for actual production

Method used

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  • Synthetic method of carbetocin acetate

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Embodiment 1

[0030] In 1963, Professor R. Bruce Merrifield published the first article on the synthesis of tetrapeptide compounds using solid-phase resin as a carrier, which made a breakthrough in the technology of peptide synthesis. For this, Professor R. Bruce Merrifield won the Nobel Prize in Chemistry in 1984.

[0031] The advantage of solid-phase synthesis is that the initial reactants and products are connected to the solid-phase carrier, so all reactions can be carried out in one reaction vessel, which is convenient for automatic operation, and high-yield products can be obtained by adding excess reactants , and the products are easily separated.

[0032] Peptide synthesis is a process of repeated addition of amino acids, and the solid-phase synthesis sequence is generally synthesized from the C-terminus (carboxyl-terminus) to the N-terminus (amino-terminus). The solid-phase synthesis method greatly reduces the difficulty of product purification in each step. In order to prevent t...

Embodiment 2

[0050] Solvent recovery and waste treatment

[0051] Solvent recovery: The solvent used in the production process is mainly N,N-dimethylformamide, which is usually collected after use.

[0052] Waste gas: The waste gas generated during the production process is mainly nitrogen gas discharged during the use of the instrument. If the nitrogen content in the air is too high, the oxygen partial pressure of the inhaled gas will drop, causing hypoxia and suffocation. When the concentration of inhaled nitrogen is not too high, the patient initially feels chest tightness, shortness of breath, and weakness; then there is irritability, extreme excitement, running around, shouting, trance, and unsteady gait, which is called "nitrogen drunk" and can enter drowsiness or comatose state. Inhalation of high concentrations can cause rapid coma and death of the patient due to respiratory and cardiac arrest. Therefore, in the production process, it is hard-sealed to provide good natural ventil...

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Abstract

The invention belongs to the technical field of amino acids, and discloses a synthetic method of carbetocin acetate. The synthetic method comprises the following steps of using Fmoc-Gly-OH and amino resin Rink Amide-MBHA Resin as starting raw materials, firstly, removing Fmoc protecting groups with a 20% DBLK solution, and performing condensation to obtain Fmoc-Gly-Rink Amide-MBHA Resin; sequentially enabling Fmoc protected amino acids to be connected, after connection, removing the Fmoc protecting groups, and performing condensation with 4-bromo butyric acid; removing Mtt protecting groups oncysteine with a weak acid system, and performing cyclization to obtain carbetocin peptide resin; and cutting the peptide resin, and purifying obtained crude peptide, to obtain pure peptide of the carbetocin. The method is simple and feasible, convenient to operate and suitable for large-scale production.

Description

technical field [0001] The invention belongs to the technical field of amino acids, and in particular relates to a synthesis method of carbetocin. Background technique [0002] At present, there have been relevant literature reports on the synthesis of carbetocin. The specific synthesis methods are generally divided into two types: liquid-phase synthesis and solid-phase synthesis. Among them, the liquid-phase synthesis has few related reports due to the difficulty of synthesis and the high cost of synthesis and purification. [0003] Patent CN102477082 A Hangzhou Hejin Technology Co., Ltd. introduces a method for synthesizing carbetocin by liquid phase synthesis. The method firstly synthesizes intermediate Ⅰ:4-Bromobutyryl-Tyr(Me)-Ile-OH, intermediate Ⅱ:H-Gln(Trt)-Asn(Trt)-Cys(Trt)-Ome and intermediate Ⅲ: H-Pro-Leu-Gly-NH 2 , The intermediates I, II, III are condensed into the non-cyclized product IV in the presence of a condensing agent in a solvent, and finally add a c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/16C07K1/16C07K1/06C07K1/04
CPCC07K7/16Y02P20/55
Inventor 王维彬胡百忠罗晓倩王美成
Owner XIANGYU PHARMA
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