Long-acting exenatide derivative, salt thereof and preparation method and application
A technology of exenatide and derivatives, applied in the field of exenatide derivatives, can solve problems such as prolonging the half-life of GLP-1, and achieve the effects of prolonging the biological half-life, prolonging the action time of hypoglycemic and weight loss, and being easy to purify
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Embodiment 1
[0049]
[0050] Synthesis
[0051] 1. Synthesis of peptide chains
[0052] 1.1 Resin swelling
[0053] Weigh 1g of 2-CTC Resin (degree of substitution 0.4mmol / g), swell with 10mL of DCM for 30min, filter to remove DCM, then swell with 10mL of NMP for 30min, rinse with NMP and 10mL of DCM respectively.
[0054] 1.2 Synthesis of Fmoc-Ser(tBu)-2-CTC Resin
[0055] Dissolve Fmoc-Ser(tBu)-OH (0.8mmol) and DIPEA (1.6mmol) in NMP10mL, then add this solution to the resin obtained in the previous step to react for 2 hours, filter the reaction solution after completion, and use DCM and NMP Wash the resin 3 times with 10 mL each.
[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, re...
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.
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