Title:
A METHOD FOR PREPARING LIRAGLUTIDE VIA A SOLID PHASE PEPTIDE SYNTHESIS
Document Type and Number:
WIPO Patent Application WO/2021/007703
Kind Code:
A1
Abstract:
Provided is a method for preparing liraglutide via a solid phase peptide synthesis, wherein the method uses a Fmoc-Gly-resin with a Fmoc protective group as a carrier for the solid phase peptide synthesis, and after the completion of a deprotecting reaction of the Fmoc protective group, each of the reactions in the solid phase peptide synthesis of the liraglutide is washed with a mixture of DMF and γ-valerolactone for several times, preferably 2-3 times.
Inventors:
BONAVENTURA IVAN DI (CN)
HE RUNZE (CN)
HE RUNZE (CN)
Application Number:
PCT/CN2019/095783
Publication Date:
January 21, 2021
Filing Date:
July 12, 2019
Export Citation:
Assignee:
SHANGHAI SPACE PEPTIDES PHARMACEUTICAL CO LTD (CN)
International Classes:
C07K14/605; C07K1/04; C07K1/06
Foreign References:
| CN102286092A | 2011-12-21 | |||
| CN103087181A | 2013-05-08 | |||
| CN103980358A | 2014-08-13 |
Other References:
JAD，Y.E.ET AL.: "Green Solid-Phase Peptide Synthesis (GSPPS) 3. Green Solvents for Fmoc Removal in Peptide Chemistry", ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 21, 30 January 2017 (2017-01-30), XP055774092, DOI: 20200320123217Y
KUMAR，A. ET AL.: "Troubleshooting When Using γ‑Valerolactone (GVL) in Green Solid-Phase Peptide Synthesis", ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 23, 3 April 2019 (2019-04-03), XP055774095, DOI: 20200320124053Y
LI，C.X. ET AL.: "Solid phase synthesis and identification of liraglutide", PRAC. J. MED. & PHARM., vol. 35, no. 6, 30 June 2018 (2018-06-30), DOI: 20200320124312Y
MA，Y.C. ET AL.: "Preparation of Liraglutide", CHINESE JOURNAL OF PHARMACEUTICALS, vol. 44, no. 2, 31 December 2013 (2013-12-31), pages 122 - 123, DOI: 20200320124443Y
KUMAR，A. ET AL.: "Troubleshooting When Using γ‑Valerolactone (GVL) in Green Solid-Phase Peptide Synthesis", ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 23, 3 April 2019 (2019-04-03), XP055774095, DOI: 20200320124053Y
LI，C.X. ET AL.: "Solid phase synthesis and identification of liraglutide", PRAC. J. MED. & PHARM., vol. 35, no. 6, 30 June 2018 (2018-06-30), DOI: 20200320124312Y
MA，Y.C. ET AL.: "Preparation of Liraglutide", CHINESE JOURNAL OF PHARMACEUTICALS, vol. 44, no. 2, 31 December 2013 (2013-12-31), pages 122 - 123, DOI: 20200320124443Y
Attorney, Agent or Firm:
KING & WOOD MALLESONS (CN)
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