Method for synthesizing Exenatide from solid phase polypeptide
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A solid-phase peptide synthesis and peptide cleavage technology, applied in the field of preparation of Exenatide, can solve the problems of limiting the large-scale production and use of Exenatide, scarcity of TentaGelS-RAM resin sources, long reaction time, etc. Easy-to-source effects
Active Publication Date: 2009-02-04
SHANGHAI SOHO YIMING PHARMA
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[0009] U.S. Patent 6,528,486 has reported the method for preparing Exenatide, is to adopt TentaGel S-RAM resin as starting material, uses DIC/HOBt or DCC/HOBt as condensation agent, and the r
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Embodiment 1
[0036] The examples and the list of raw materials used in the foregoing process are as follows:
[0037] No
Raw material and prototype name
Source
1
Rink Amide resin
Tianjin Hecheng Technology Co., Ltd.
2
Rink Amide AM resin
Tianjin Hecheng Technology Co., Ltd.
3
Rink Amide MBHA resin
Tianjin Hecheng Technology Co., Ltd.
4
Fmoc-Ala-OH
Suzhou Tianma Pharmaceutical Group
5
Fmoc-Arg(Pbf)-OH
Suzhou Tianma Pharmaceutical Group
6
Fmoc-Asn(Trt)-OH
Suzhou Tianma Pharmaceutical Group
7
Fmoc-Asp(OtBu)-OH
Suzhou Tianma Pharmaceutical Group
8
Fmoc-Gln(Trt)-OH
Suzhou Tianma Pharmaceutical Group
9
Fmoc-Glu(OtBu)-OH
Suzhou Tianma Pharmaceutical Group
10
Fmoc-Gly-OH
Suzhou Tianma Pharmaceutical Group
11
Fmoc-His(Trt)-OH
Suzhou Tianma Pharmaceutical Group
12
Fmoc-Ile-OH
Suzhou Tia...
Embodiment 2
[0126] The same method and process conditions as in Example 1 are adopted, in which:
[0127] Using RinkAmide AM resin as the starting material, after swelling with DMF, add Fmoc-Ser(tBu)-OH, TBTU, HOBt, and dissolve the mixture with peptide reagent, react at 25°C for 2 hours, and wash with DMF and absolute ethanol three times respectively.
[0128] Add decapping reagent and react for 0.5 hour at 25°C. After sufficient washing, add Fmoc-amino acid, TBTU / HOBt or HBTU / HOBt or BOP / HOBt mixture dissolved with peptide reagent, and react at 25°C for 1 hour. The operation is the same as in Example 1. , Until the thirty-nine peptide is received. After cleavage of peptides and other reactions, 10.6 g of white loose lumps are obtained.
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Abstract
The invention discloses a preparation method of solid phase peptide synthesis Exenatide which includes the following steps: taking Rink Amide resins, Rink Amide AM resins or Rink Amide MBHA resins as starting materials, amino acids with Fmoc protective groups are sequentially connected, so as to obtain protective thirty-nine peptide resins; and meanwhile, after thirty-nine peptide resins are obtained by sequentially removing Fmoc-protective groups and transpeptidase reactions by condensing agents, acellular side-chain protective groups and cutting peptides are carried out sychronously to obtain Exenatide crude products, and then products (comprising medical salts and free alkali, such as acetates, trifluoroacetate, etc.) are obtained after Exenatide crude products are separated and purified by C18 or C8 column and freeze-dried. The preparation method has the advantages of stable technology, conventient raw and auxiliary material sources, short production cycle, low production cost, few three wastes, high yield, stable yield, stable quality, low production cost and high yield.
Description
Technical field [0001] The present invention relates to a preparation method of Exenatide, in particular to a preparation method of solid-phase polypeptide synthesis Exenatide. Background technique [0002] Chinese name: Exenatide, Exenatide acetate. [0003] Product name: BYETTA . English name: Exenatide Acetate. [0004] Structural formula: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu- Trp(Boc)-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH 2 [0005] The molecular formula is: C 184 H 282 N 50 O 60 S [0006] The molecular weight is: 4186.6 [0007] Diabetes is a worldwide disease. There are more than 150 million diabetic patients in the world, among which 90% are type II diabetic patients. [0008] There are nearly 40 million type II diabetes patients in my country. With the improvement of living standards, the incidence rate will be higher and higher. There are more cities than rural areas. Because patients have...
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