Preparation method of liraglutide

A technology of liraglutide and liraglutide, which is applied in the field of preparation of liraglutide, can solve the problems of low amino acid access rate and reduced yield, and achieve the reduction of purification difficulty, production cost and preparation cost low effect
CN107056927AActive Publication Date: 2017-08-18SICHUAN JISHENG BIOPHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SICHUAN JISHENG BIOPHARM CO LTD
Publication Date
2017-08-18

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Abstract

The invention discloses a preparation method of liraglutide. The preparation method comprises the following steps: using a deprotection reagent Fmoc-Gly-wang resin for deprotection, and removing Fmoc protective groups; coupling three protective amino acids at the 12th-14th sites by protective peptide fragments X; coupling three protective amino acids at 20-22 sites by protective peptide fragments Y; coupling protective amino acid at the 31th site by a Boc-His(trt)-OH protective form; removing alloc protection of lysine side chains for main-chain peptide resin of the liraglutide, coupling the side chains one by one and thus obtaining peptide resin of the liraglutide; cracking the peptide resin of the liraglutide in cracking liquid and thus obtaining a liraglutide crude product; purifying the liraglutide crude product and thus obtaining a liraglutide fine product. The preparation method disclosed by the invention has the advantages that segment coupling is carried out on amino sites which are easiest for folding in the process of synthesizing the main chain of the liraglutide, so that the problems of multiple times of coupling and low access rate for the amino acids due to folding in the synthesis process are avoided, the production cycle of the liraglutide is shortened, and the synthetic yield of the liraglutide is increased.
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Description

technical field

[0001] The present invention relates to the synthesis of polypeptides, in particular to a preparation method of liraglutide. Background technique

[0002] At present, with the improvement of living standards, the number of people suffering from diabetes is gradually increasing, and liraglutide, a human glucagon-like peptide-1 (GLP-1) analogue, is used for the treatment of diabetes. The structure of liraglutide is: His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(Na- PAL-γ-Glu)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH. Therefore, there is a great demand for liraglutide in the market. There are many synthetic methods available. The method of genetic engineering is difficult and technically difficult; during the synthesis process, the most easily foldable amino sites (20-22 and 12-14) in the main chain synthesis process are likely to cause amino folding, resulting in by-products. The product and other impurities affect th...

Claims

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