Long-acting Exenatide Derivatives and Salts, Preparation Methods and Applications
A technology of exenatide and its derivatives, which is applied in the field of exenatide derivatives, can solve the problems of prolonging the half-life of GLP-1, achieve the goal of reducing blood sugar and slowing down, low production cost, and prolonging the time of hypoglycemic and weight loss. Effect
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0049]
[0050] Synthesis
[0051] 1. Synthesis of Peptide Chains
[0052] 1.1 Resin swelling
[0053] Weigh 1 g of 2-CTC Resin (degree of substitution 0.4 mmol / g), swell with 10 mL of DCM for 30 min, filter to remove DCM, then swell with 10 mL of NMP for 30 min, rinse with NMP and 10 mL of DCM respectively.
[0054] 1.2 Synthesis of Fmoc-Ser(tBu)-2-CTC Resin
[0055] Dissolve Fmoc-Ser(tBu)-OH (0.8 mmol) and DIPEA (1.6 mmol) in 10 mL of NMP, and then add this solution to the resin obtained in the previous step to react for 2 hours. and NMP 10 mL each to wash the resin 3 times.
[0056] 1.3 Removal of Fmoc protecting group
[0057] 25% piperidine / NMP (V / V) solution containing 0.1 M HOBt was added to the washed resin to remove Fmoc. After the reaction, the resin was washed 3 times with 10 mL each of DCM and NMP.
[0058] 1.4 Peptide chain extension
[0059] According to the sequence of the exenatide derivative peptide chain, repeat the above deprotection and coupling st...
Embodiment 2
[0067]
[0068] The synthesis method was the same as in Example 1, and the collected solution was lyophilized to obtain 24.9 mg of the pure product. The theoretical relative molecular mass is 8654.6. ESI-MS m / z: Calcd. [M+5H] 5+ 1731.9, [M+6H] 6+ 1443.4; Found [M+5H] 5+ 1732.1,[M+6H] 6+ 1443.7.
Embodiment 3
[0070]
[0071] The synthesis method was the same as in Example 1, and the collected solution was lyophilized to obtain 26.5 mg of the pure product. The theoretical relative molecular mass is 8738.8. ESI-MS m / z: Calcd. [M+5H] 5+ 1748.8, [M+6H] 6+ 1457.5; Found [M+5H] 5+ 1748.9,[M+6H] 6+ 1458.0.
PUM
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com