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A kind of synthetic method of ularitide

A technology of uralipide and a synthesis method, applied in the field of medicine, can solve problems such as environmental protection unfavorable to green chemistry, difficulty in dissolving uralipide, unfavorable large-scale production, etc., so as to shorten the oxidation reaction time, avoid the generation of organic waste liquid, realize The effect of mass production

Inactive Publication Date: 2020-02-04
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, using this scheme for oxidation, due to the difficulty in dissolving uraritide and the final oxidation needs to be carried out at a very dilute concentration, the operation is very difficult, and the reaction time is long, which is not conducive to large-scale production
In addition, this method will produce a large amount of mixed waste liquid of organic solvent and water, which is not conducive to the requirements of green chemistry in terms of environmental protection.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Preparation of Uralitide Linear Peptide Crude Peptide

[0044] By means of solid phase synthesis one by one, 1 mol of ularitide was synthesized to obtain 3510 g of crude peptide, the yield of crude peptide was 100.1%, and the purity was 78.43%.

Embodiment 2

[0045] Example 2: Oxidation reaction of crude peptide of ularitide linear peptide

[0046] Take 100 g of the crude linear peptide obtained in Example 1, dissolve it in 5.0 L of [C2mim][OAc] (the oxidation concentration is 20 mg / mL), adjust the pH of the solution to an alkaline environment of 7.0-7.5 with ammonia water, stir slightly at room temperature, After 2.0 hours of oxidation reaction, 0.5 L of 0.1% TFA aqueous solution was added to adjust the pH value of the solution to be acidic, and the oxidation was completed, and the purity of the crude product of ularitide was 62.47%.

Embodiment 3

[0047] Example 3: Oxidation reaction of crude peptide of ularitide linear peptide

[0048] Take 100 g of the crude linear peptide obtained in Example 1, dissolve it in 5.0 L of [C2mim] [TFA] (the oxidation concentration is 20 mg / mL), adjust the pH of the solution to 7.0-7.5 alkaline environment with ammonia water, stir slightly at room temperature, After 2.0 hours of oxidation reaction, 0.5 L of 0.1% TFA aqueous solution was added to adjust the pH value to be acidic, and the oxidation was completed. The purity of the crude product obtained from ularitide was 76.81%.

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Abstract

The invention relates to the technical field of medicament, and discloses a synthetic method for ularitide. According to the synthetic method, ularitide linear peptide crude peptide or fine peptide is added in ionic liquid with the melting point below 20 DEG C, oxidization is conducted for 0.5-3 h in the alkaline environment, and a disulfide bond ularitide crude product is obtained. According to the synthetic method, the room temperature ionic liquid carrier is used for replacing an organic solvent and water liquid phase oxidizing medium in the traditional oxidization link, the crude peptide purity of the ularitide obtained through solid-phase synthesis and the total fine peptide yield are obviously increased, meanwhile, the oxidization reaction time can be greatly shortened, operation is convenient, and generation of organic waste liquid is avoided.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for synthesizing ularitide. Background technique [0002] Ularitide is a natriuretic peptide isolated from human urine. Its analytical structure is similar to that of atrial natriuretic peptide, except that there are four more amino acid residues at the N-terminal of its sequence. Relevant studies have shown that Ularitide has various effects such as dilating blood vessels, dilating bronchi and diuresis, and has certain therapeutic effects on heart failure, renal failure, pulmonary hypertension and bronchial asthma clinically. [0003] The structure of Uralitide is a polypeptide composed of 32 amino acids containing a pair of intramolecular disulfide bonds, which is generally prepared by chemical synthesis. The sequence structure is: [0004] H-Thr-Ala-Pro-Arg-Ser-Leu-Arg-Arg-Ser-Ser-Cys-Phe-Gly-Gly-Arg-Met-Asp-Arg-Ile-Gly-Ala-Gln-Ser-Gly- Leu-Gly-Cys-Asn-Ser-Phe-Arg-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/58C07K1/20C07K1/06C07K1/04
CPCC07K14/58
Inventor 戴政清宓鹏程伍柯瑾陶安进袁建成
Owner HYBIO PHARMA
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