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Method for preparing oxytocin

The technology of oxytocin and condensing agent is applied in the field of preparation of oxytocin, which can solve the problems of low total yield and complicated processing process, and achieve the effects of complete peptide linkage, high chemical purity and high yield.

Active Publication Date: 2008-08-06
YANCHENG KAILI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this process ensures the optical purity of the target product, the process is cumbersome and the total yield is low

Method used

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  • Method for preparing oxytocin
  • Method for preparing oxytocin
  • Method for preparing oxytocin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The preparation of embodiment 1 intermediate a

[0051] Take 0.1 mol of cysteinyl tyrosine (dipeptide, a1) and isoleucyl glutamic acid (dipeptide, a2), 0.1 mol of DEPBT, dissolve in 500ml of DMF, and control the temperature at 30°C , reacted for 2 hours, removed DMF under vacuum conditions (vacuum degree is not more than 10mmHg), then added 30% sodium hydroxide solution 200ml, controlled saponification temperature 30 ° C, saponification reaction time 1 hour, obtained intermediate a.

Embodiment 2

[0052] The preparation of embodiment 2 intermediate b

[0053] Take 0.1 mol of pentapeptide resin b1, add 600ml of anisole, control the reaction temperature to 30°C, and the reaction time to 1 hour, filter and remove the resin to obtain intermediate b.

Embodiment 3

[0054] The preparation of embodiment 3 oxytocin

[0055] Combine the products obtained in Example 1 and Example 2, add 300ml of DMF, 120ml of DPPA, and 100ml of dioxane, control the reaction temperature to 10°C, and the reaction time to 24 hours. After the reaction finishes, filter and rinse with an appropriate amount of dioxane / water, then add 100ml of TFA (30%), 400ml of DCM to the filter residue, control the reaction temperature at 0°C, and the reaction time for 2 hours; then add 500ml of piperidine ( 50%) and 500ml of DMF, feed enough air, control the reaction temperature is not more than 10 ℃, the reaction time is 3 hours, remove the solvent under vacuum conditions (vacuum degree is not more than 10mmHg), obtain the target product oxytocin.

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Abstract

The invention discloses an oxytocin preparation method which comprises respectively synthesizing intermediate a and intermediate b, using diphenyl azidophopshate as condensing agent, in the presence of DMF, DPPA, dioxane, piperidine, TFA and DCM, to react the intermediates a, b, controlling the reaction temperature at -20-40DEG C and reaction time of 10-40h, feeding air, after the oxidization, drying in vacuum to remove the solvent in the reaction system to obtain oxytocin. The invention has complete connected peptide chain, simple purification, simple process, high yield, high optical activity and chemical purity of target product oxytocin.

Description

technical field [0001] The present invention relates to the preparation method of medicine, specifically, the present invention is a kind of preparation method of oxytocin. Background technique [0002] Oxytocin (OXYTOCIN), also known as oxytocin, is a biologically active polypeptide amino acid product composed of 9 amino acid residues. Oxytocin can not only be used to induce labor for women of childbearing age, but also widely used in the animal and plant breeding industry in the world. If it is used in animals, it can not only improve the conception rate and reproduction rate of animals, but also improve the fertility of animals. unit milk yield; when used on fruit trees, it can not only enhance the excellent appearance of the fruit, but also play a role in accelerating ripening. [0003] At present, the preparation methods of oxytocin include liquid-phase synthesis and solid-phase synthesis. [0004] The liquid-phase synthesis method has adopted the benzyloxycarbonyl (C...

Claims

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Application Information

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IPC IPC(8): C07K7/16C07K1/10
Inventor 吴永平
Owner YANCHENG KAILI PHARMA
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