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Title:
PREPARATION METHOD FOR SEMAGLUTIDE
Document Type and Number:
WIPO Patent Application WO/2021/143073
Kind Code:
A1
Abstract:
A preparation method for semaglutide. The method comprises: producing a semaglutide resin by means of a solid-phase synthesis, producing crude semaglutide by cleavage and deprotection, producing refined semaglutide by purification and freeze-drying, comprising the solid-phase synthesis of a semaglutide 1-6 peptide fragment resin, which is cleaved and purified to serve as a first peptide fragment; and synthesizing a lysine having a sidechain group at locus 20 of semaglutide to serve as a second peptide fragment. In the method, prepared is a semaglutide loci 1-6 fully protected peptide fragment, which serves as a key starting material applied in the solid-phase synthesis of semaglutide, thus reducing the generation of D-His, D-Glu, D-Thr, D-Phe racemic impurities and +Gly impurities, reducing the difficulty of coarse product purification, increasing the purity and yield of semaglutide, reducing synthesis costs, and favoring industrialized large-scale production.

Inventors:
LI XINYU (CN)
FU YUQING (CN)
ZHANG LIXIANG (CN)
YAO LIN (CN)
LI WENJING (CN)
Application Number:
PCT/CN2020/101081
Publication Date:
July 22, 2021
Filing Date:
July 09, 2020
Export Citation:
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Assignee:
SHENZHEN JYMED TECH CO LTD (CN)
International Classes:
C07K14/605; C07K1/04; C07K1/06
Domestic Patent References:
WO2018032843A12018-02-22
WO2019069274A12019-04-11
WO2018032521A12018-02-22
Foreign References:
CN109456401A2019-03-12
CN106749613A2017-05-31
CN104356224A2015-02-18
CN110372785A2019-10-25
CN109627317A2019-04-16
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