Hybio Pharmaceutical Co., Ltd.

Yaping Ma

Jiancheng Yuan

Jian Hua Liu

Jian Hui Liu

Jian Liu

Pengcheng Mi

Junfeng Pan

Qing Xiao

Youjin Chen

Guotao Li

Huixing Yuan

Xu Kang

Hongling Li

Liangzheng Qin

Disclosed is a method for preparing ganirelix acetate. The method includes the following steps: respectively replacing Fmoc-HArg(Et)-OH and Fmoc-D-HArg(Et)-OH by employing Fmoc-Lys(Boc)-OH and Fmoc-D-Lys(Boc)-OH or Fmoc-Lys(Alloc)-OH and Fmoc-D-Lys(Alloc)-OH; synthesizing a ganirelix precursor I or ganirelix precursor II-peptide resin in advance; and then respectively performing modifications and treatments on side chain amino groups of Lys and D-Lys in the precursor I or the precursor II-peptide resin to obtain ganirelix acetate. The ganirelix acetate synthesized therefrom is high in purity, has few impurities and a relatively low cost, and is suitable for large-scale production.

Ganirelix precursor and method for preparing ganirelix acetate by using the same

The present invention discloses a method for preparing glatiramer acetate, comprising: (1) dissolving L-alanine NCA, L-tyrosine NCA, L-glutamic acid-&#x3b3;-benzyl ester NCA, and L-&#x3b5;-trifluoroacetyl-lysine NCA in 1,4-dioxane as solvent, stirring until a clarified solution is formed; (2) adding diethylamine for catalysis, stirring at 20-25&#xb0; C., then slowly pouring the reaction solution into water, collecting the produced white product; (3) adding the obtained product to a solution of hydrobromic acid in acetic acid, stirring at 23.0-25.0&#xb0; C., pouring the reaction solution into purified water for quenching and stirring, subjecting the mixture to suction filtration to obtain a yellow solid, after repeating 3-5 times, subjecting the solid to blast drying to remove the moisture therein; and (4) dissolving the solid obtained in step (3) in a 1M piperidine aqueous solution at room temperature and stirring, subjecting the obtained solution to dialysis, adding glacial acetic acid to adjust the pH to 5.5-7.0, and lyophilizing.

Method for preparing glatiramer acetate

Disclosed in the present invention is a method for preparing Exenatide. Serine resin is obtained through a first coupling of serine and resin and successively with amino acids through a second coupling to obtain a peptide resin with a sequence as shown by SEQ ID No. 1; Exenatide resin is obtained through a third coupling of histidine containing a protecting group or salts thereof and the peptide resin with a sequence as shown by SEQ ID No. 1, then it is cracked and purified to obtain purified Exenatide peptide. The method for preparing Exenatide of the present invention inhibits the formation of D-His-Exenatide, and thereby improves the yield and purity of Exenatide.

Method for preparing exenatide

Provided is a method for preparing eptifibatide, wherein the method comprises: obtaining an eptifibatide refined peptide solution; and obtaining and freeze-drying an eptifibatide refined peptide concentrate after rotary evaporation of the eptifibatide refined peptide solution, wherein the concentration of the eptifibatide refined peptide concentrate is 15-30 mg/ml and the temperature of rotary evaporation is 251&#xb0; C.-35&#xb0; C. The preparation method of the eptifibatide refined peptide solution is as follows: coupling Cys with a resin to obtain a Cys-resin; obtaining a polypeptide having a sequence as represented by SEQ ID NO: 1 by gradually coupling the Cys-resin with Pro, Trp, Asp, Gly, Har and Mpa; and obtaining the eptifibatide refined peptide solution through oxidation, cleavage, purification and transfer to salt.

Method for preparing eptifibatide

The present invention provides a method for preparing atosiban acetate. The method comprises the following steps of: synthesizing to obtain linear atosiban; dissolving the linear atosiban in an acetonitrile aqueous solution, adjusting the pH value with ammonia water, adding HOfor oxidizing, filtering, purifying, and transferring salt to obtain the atosiban acetate. In the present invention, an appropriate route is provided, the linear atosiban is synthesized by adopting a solid phase method, and the atosiban is obtained by liquid phase oxidation. The method has the advantages of capabilities of solving the problem of insolubility of the linear atosiban, reducing the reaction size to the maximum extent and shortening reaction time, and being high in yield and easy to industrialize.

Method for preparing atosiban acetate

Provided is a method for solid phase synthesis of liraglutide, comprising the following steps: A), Fmoc-Gly-resin being obtained by coupling resin solid phase carrier with glycine with N-end protected by Fmoc(Fmoc-Gly-OH) in the presence of activator system; B) according to the peptide sequence of the main chain of liraglutide, successively coupling with amino acids with N-ends protected by Fmoc and protected side chains by the method for solid phase synthesis, wherein lysine employs Fmoc-Lys(Alloc)-OH; C) removing the protective group, Alloc, from the side chain of lysine; D) coupling the side chain of lysine with Palmitoyl-Glu-OtBu by the method for solid phase synthesis; E) cleavage, removing protection groups and resin to obtain crude liraglutide; F) purifying and lyophilizing to obtain liraglutide.

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Shenzhen, China

Yaping Ma