Title:
METHOD FOR SYNTHESIZING C-TERMINAL PROTECTION FRAGMENT OF PEPTIDE
Document Type and Number:
WIPO Patent Application WO/2022/134124
Kind Code:
A1
Abstract:
The present invention relates to the field of polypeptide synthesis, and provides a method for synthesizing the C-terminal protection fragment of a peptide. The method comprises the following steps: (1) preparing Resin-T-P; and (2) removing resin by means of using a lysis reagent to obtain a T-P. The loading of amino acids is realized by means of using a medium-acid sensitive connecting arm as a secondary connecting arm and reacting same with an acid-sensitive resin or a nucleophilic sensitive resin and Fmoc-AA-OH. Then, the assembly of the peptide chain is completed. After the assembly of the peptide chain is completed, a strong acid or a nucleophilic reagent is used to cleave the resin, and the protective peptide fragment and the secondary connecting arm are simultaneously released as an integral molecule. By means of using the method, a C peptide protection fragment with a protecting group at a release terminal can be directly released from a solid phase, and the protection fragment can be directly used for the synthesis of a polypeptide or a polypeptide fragment containing carboxyl at the C-terminal. The method reduces the preparation steps, improves the synthesis yield, greatly reduces the risk of racemization, and has low costs, it is easy to control the reaction, and same can also be used for large-scale production.
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Inventors:
WANG GANG (CN)
SHU SUIZHI (CN)
ZHANG LIXIANG (CN)
LI XINYU (CN)
YUE ZELE (CN)
SHU SUIZHI (CN)
ZHANG LIXIANG (CN)
LI XINYU (CN)
YUE ZELE (CN)
Application Number:
PCT/CN2020/139775
Publication Date:
June 30, 2022
Filing Date:
December 26, 2020
Export Citation:
Assignee:
SHENZHEN JYMED TECH CO LTD (CN)
International Classes:
C07K1/02; C07K1/10; C07K14/605
Foreign References:
| US20200024306A1 | 2020-01-23 | |||
| CN103709243A | 2014-04-09 | |||
| CN112010961A | 2020-12-01 | |||
| CN103467595A | 2013-12-25 | |||
| US20170029467A1 | 2017-02-02 |
Other References:
MA YANCHI,DONG YUANZHEN,ZHANG XIQUAN,FENG JUN: "Preparation of Liraglutide", CHINESE JOURNAL OF PHARMACEUTICALS, vol. 44, no. 2, 10 February 2013 (2013-02-10), pages 121 - 124, XP055946164, ISSN: 1001-8255, DOI: 10.16522/j.cnki.cjph.2013.02.017
S. MERANI, W. TRUONG, J. A. EMAMAULLEE, C. TOSO, L. B. KNUDSEN, A. M. J. SHAPIRO: "Liraglutide, a Long-Acting Human Glucagon-Like Peptide 1 Analog, Improves Glucose Homeostasis in Marginal Mass Islet Transplantation in Mice", ENDOCRINOLOGY, vol. 149, no. 9, 1 September 2008 (2008-09-01), pages 4322 - 4328, XP055114009, ISSN: 00137227, DOI: 10.1210/en.2008-0501
S. MERANI, W. TRUONG, J. A. EMAMAULLEE, C. TOSO, L. B. KNUDSEN, A. M. J. SHAPIRO: "Liraglutide, a Long-Acting Human Glucagon-Like Peptide 1 Analog, Improves Glucose Homeostasis in Marginal Mass Islet Transplantation in Mice", ENDOCRINOLOGY, vol. 149, no. 9, 1 September 2008 (2008-09-01), pages 4322 - 4328, XP055114009, ISSN: 00137227, DOI: 10.1210/en.2008-0501
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