Glucagon-like peptide 1 (GLP-1) analogues with long-acting effect and application thereof
A technology of glucagon and GLP-1, which is applied in the field of glucagon-like peptide-1 analogs, can solve the problems of GLP-1 loss of biological activity and loss of histidine residues, etc. Sugar effect, chemically stable effect
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[0095] Example 1
[0096]
[0097] Microwave promoted solid phase synthesis
[0098] (1) Synthesis of cysteine modified by fatty chain
[0099] Weigh 0.21g of Fmoc-Cys-OH, dissolve it in DCM, add 0.12g of N-octylmaleimide, 3ul DIEA as a catalyst, and stir the reaction at room temperature. After the reaction is monitored by the thin-layer plate, the reaction solution is reduced. It was concentrated by pressure and separated by column chromatography to obtain 0.26 g of product with a yield of 78%.
[0100] MS(70eV)m / z: 575.5([M+Na] + ).
[0101] (2) Swelling of resin
[0102] Weigh 50mg of Fmoc-Rink amide-MBHA Resin (substitution amount 0.4mmol / g), swell with 7mL DCM for 30min, suction filter to remove DCM, swell with 10mL NMP for 30min, and finally rinse with NMP, DCM, NMP 7mL respectively.
[0103] (3) Microwave promotes the removal of Fmoc protecting group
[0104] Put the swollen resin into the reactor, add 7 mL of 25% piperidine / NMP(V / V) solution containing 0.1M HOBT, and react in a ...
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[0117] Examples 2-12
[0118] According to the general method described in Example 1, the glucagon-like peptide-1 (GLP-1) analogues of Examples 2-12 were synthesized according to the corresponding sequence, and they were confirmed by electrospray mass spectrometry (ESI-MS). The molecular weight.
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[0119] Example 2
[0120]
[0121] The theoretical relative molecular mass is 3566.1. ESI-MS m / z: found[M+4H] 4+ 892.5, [M+5H] 5+ 714.2; calu[M+4H] 4+ 892.1, [M+5H] 5+ 713.9
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