Invention Grant
- Patent Title: Synthesis method for liraglutide with low racemate impurity
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Application No.: US16326265Application Date: 2017-08-18
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Publication No.: US11518794B2Publication Date: 2022-12-06
- Inventor: Yuqing Fu , Hongji Ma , Xinyu Li , Lixiang Zhang , Qin Zhi , Lifen Wu , Zicheng Liu
- Applicant: SHENZHEN JYMED TECHNOLOGY CO., LTD.
- Applicant Address: CN Shenzhen
- Assignee: SHENZHEN JYMED TECHNOLOGY CO., LTD.
- Current Assignee: SHENZHEN JYMED TECHNOLOGY CO., LTD.
- Current Assignee Address: CN Shenzhen
- Agency: Kagan Binder, PLLC
- Priority: WOPCT/CN2016/096118 20160819
- International Application: PCT/CN2017/097970 WO 20170818
- International Announcement: WO2018/033127 WO 20180222
- Main IPC: C07K14/605
- IPC: C07K14/605 ; C07K1/04 ; C07K1/06

Abstract:
A synthesis method for low-racemization impurity liraglutide comprises the following steps: performing synthesis to obtain a propeptide, coupling 2 to 5 peptides comprising Thr-Phe on the propeptide by using a solid-phase synthesis method; further, performing solid-phase synthesis to obtain a liraglutide resin; the liraglutide resin is cracked after modification, or the liraglutide resin is directly cracked, purified and frozen dry, so as to obtain the liraglutide. The provided liraglutide synthesis method effectively restrains or reduces the generation of racemization impurity D-Thr5 highly similar to a product property, which facilitates the purification of the coarse liraglutide, and the high yield of the liraglutide is ensured, thereby greatly reducing production costs; during the synthesis of the liraglutide, the syntheses between dipeptide fragments, tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly-resin or the syntheses between the combination of the dipeptide fragments, the tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly resin can be carried out at the same time, and accordingly the synthesis time is shortened to some extent.
Public/Granted literature
- US20190211073A1 SYNTHESIS METHOD FOR LIRAGLUTIDE WITH LOW RACEMATE IMPURITY Public/Granted day:2019-07-11
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