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Semaglutide sodium salt as well as preparation method and application thereof

A technology of semaglutide sodium salt and semaglutide, which is applied in the field of semaglutide sodium salt and its preparation, can solve the problems of easily missing carbon-terminal amino acids, difficult control of polymer impurities, and difficulty in amino acid coupling , to achieve the effect of facilitating large-scale industrial production, improving convenience, and easy control of the process

Pending Publication Date: 2022-02-11
ZHEJIANG PEPTITES BIOTECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the synthesis of semaglutide has the following problems: difficult coupling of individual amino acids in the semaglutide sequence, easy deletion of carbon-terminal amino acids, low purity of crude peptide, large number of impurities, and difficulty in separation and purification.
In addition, the stability of the trifluoroacetate and acetate forms of semaglutide reported so far is relatively poor, and the polymer impurities are difficult to control. These factors are not conducive to industrial production.

Method used

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  • Semaglutide sodium salt as well as preparation method and application thereof
  • Semaglutide sodium salt as well as preparation method and application thereof
  • Semaglutide sodium salt as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0143] 1.1 Synthesis of semaglutide peptide resin

[0144] Weigh AM Resin (3.8g, 2mmol, degree of substitution 0.53mmol / g) into the reactor, swell with 200ml of 5% (v / v) DIPEA in DMF, and remove the liquid by suction filtration. Wash 4 times with 50ml of DMF, drain the solvent, and use ninhydrin to do the positive amino group test to prove the existence of free amino groups.

[0145] In addition, weigh Fmoc-N (Gly-O t Bu) Hmb Butyric Acid (3.45g, 6mmol) and HOBt (0.81g, 6mmol) were added to a beaker, dissolved in 20ml of DMF, the temperature was controlled at 10°C, and DIC (0.94ml, 6mmol) was added to preactivate the reaction for 10min. Add the pre-activation solution into the reactor and stir for 2 hours. Use ninhydrin as a qualitative detection of amino groups to track the end of the reaction. If the reaction solution is colorless and transparent, it means that the test is negative, indicating that the reaction is complete. The liquid was removed by suction filtration, and...

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Abstract

The invention discloses a semaglutide sodium salt as well as a preparation method and application thereof. The molar ratio of sodium ions to semaglutide in the semaglutide sodium salt is (1-7):1. Compared with other salt forms, the stability of the semaglutide sodium salt is greatly improved.

Description

technical field [0001] The application relates to a sodium salt of semaglutide and its preparation method and application, belonging to the technical field of diabetes drugs. Background technique [0002] Diabetes is a global disease. According to reports, in 2014, there were 422 million diabetics in the world, accounting for about 8.5% of the global population, of which type II diabetes accounted for about 90%. Semaglutide is a modification of human glucagon-like peptide-1 (GLP-1) used for the treatment of type II diabetes. Points and immunogenicity are similar to GLP-1. [0003] The English name of semaglutide is semaglutide, and its sequence is: [0004] His 1 -Aib 2 -Glu 3 -Gly 4 -Thr 5 -Phe 6 -Thr 7 -Ser 8 -Asp 9 -Val 10 -Ser 11 -Ser 12 -Tyr 13 -Leu 14 -Glu 15 -Gly 16 -Gln 17 -Ala 18 -Ala 19 -Lys 20 (PEG2-PEG2-γ-Glu-Octadecanedioic)-Gl u 21 -Phe 22 -Ile 23 -Ala 24 -Trp 25 -Leu 26 -Val 27 -Arg 28 -Gly 29 -Arg 30 -Gly 31 . [0005] Semagl...

Claims

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Application Information

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IPC IPC(8): C07K14/605C07K1/20C07K1/30C07K1/04C07K1/06C07K1/36A61K38/26A61P3/10
CPCC07K14/605A61K38/26A61P3/10Y02P20/55
Inventor 刘志国张启鹏刘慧敏
Owner ZHEJIANG PEPTITES BIOTECH CO LTD
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