A kind of method for preparing alendidil

A synthesis method and technology of peptide fragments, applied in the field of polypeptide drug preparation, can solve problems such as low synthesis efficiency, unsuitability for large-scale production, and high cost of histidine racemization
CN104447963BActive Publication Date: 2017-11-07ADLAI NORTYE BIOPHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ADLAI NORTYE BIOPHARMA CO LTD
Publication Date
2017-11-07

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Abstract

The invention relates to the technical field of polypeptide synthesis, and in particular relates to a method for preparing aviptadil. The method specifically comprises the following steps: (A) synthesizing a dipeptide fragment Fmoc-Leu-Asn-OH by virtue of a liquid phase method; (B) sequentially coupling amino acids with N end Fmoc protection and side chain protection according to an aviptadil main chain peptide sequence by adopting a solid phase synthesis method and taking Rink Amide MBHA amino resin as initial resin, wherein the amino acid coupling of 23, 24, 27 and 28 positions is realized by adopting the dipeptide fragment Fmoc-Leu-Asn-OH coupling, and the histidine coupling of a first position is realized by adopting Boc-His(Trt)-OH; and (C) performing peptide resin pyrolysis, purification and freeze-drying to obtain aviptadil. The invention provides D-His1-aviptadil which is high in synthetic efficiency and low in cost and can avoid racemization impurities, so that the method is suitable for a synthetic process of aviptadil in scale production.
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Description

technical field

[0001] The invention belongs to the technical field of preparation methods of polypeptide drugs, and in particular relates to a method for preparing alendidel. Background technique

[0002] Aviptadil, British name: Aviptadil.

[0003] The peptide sequence of the alendidil is as follows:

[0004] H-His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn- Ser-Ile-Leu-Asn-NH 2

[0005] Altideil, developed for Mondobiotech AG and Biogen Idec, is a linear peptide of 28 amino acids. It is mainly used for the treatment of acute respiratory distress syndrome and idiopathic pulmonary fibrosis. It has better effect and less side effects, and is a promising peptide drug.

[0006] At present, the conventional synthesis method of alendidil is a one-by-one coupling method, and the synthesis efficiency is low, and the coupled histidine is easy to racemize; in addition, CN201310100852.3 reports the use of Boc-His(3-Bum)-Ser(Psi(Me...

Claims

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