Synthesis method for liraglutide with low racemate impurity
US11518794B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 18, 2017 |
| Grant date | Dec 6, 2022 |
| Priority date | — |
| Expiry date | Apr 7, 2040 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K14/001
- WIPO fieldBiotechnology
- WIPO sectorChemistry
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 tim…
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