Solid-phase synthesis method for preparing exenatide
A technology for exenatide and solid-phase synthesis, which is applied in the preparation methods of peptides, chemical instruments and methods, peptides, etc., can solve the problems of complex synthesis steps, difficult separation in the later stage, and difficult coupling, etc., and achieves reduction of residual peptides. The formation of impurities, the elimination of β-sheet secondary space structure, and the effect of improving yield
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[0061] Example 1
[0062] (1) Preparation of Fmoc-Rink Amide AM PEGMatrix resin
[0063] Weigh 25 grams (0.8mmol / g, 20mmol) of AM PEGMatrix resin, soak it in 500ml DCM for 30 minutes to fully swell the resin, drain it, and add Fmoc-Rink Amide linker (MW:539.58, 40mmol) 21.6g, DIEA (MW : 129.24, 80mmol) 13.5ml, TBTU (MW: 321.1, 40mmol) 12.8g, HOBT (MW: 135.1, 40mmol) 5.4g, DMF / NMP 500ml with a volume ratio of 1:1, react for 4 hours, drain it, and use DMF Wash 3 times, drain dry, then add 500ml of acetic anhydride:pyridine:DMF mixed solution with a volume ratio of 2:2:1, react for 1 hour, drain dry, wash 6 times with DMF, drain dry to obtain Fmoc-RinkAmide AM PEGMatrix Resin.
[0064] (2) Preparation of His(trt)-Gly-Glu(otbu)-{Gly-Thr(psi(me,me)pro)}-Phe-Thr(tbu)-Ser(tbu)-Asp(otbu)-{Leu -Ser(psi(me,me)pro))-Lys(boc)-Gln(trt)-Met-Glu(otbu)-Glu(otbu)-Glu(otbu)-Ala-Val-Arg(pbf)-Leu -Phe-Ile-Glu(otbu)-Trp(boc)-Leu-Lys(boc)-Asn(trt)-Gly-Gly-Pro-{Ser(tbu)-Ser(psi(me,me)pro)} -Gly-Ala-Pr...
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[0106] Example 2
[0107] Step (1) AM PEGMatrix resin reacts with Fmoc-Rink Amide linker and DIEA for 8 hours, then add acetic anhydride: pyridine: DMF mixed solution to react for 0.5 hours, PEGMatrix resin substitution degree is 1.0mmol / g; Step (2) Fmoc -Rink Amide AM PEGMatrix resin, add deprotection reagent, react for 45 minutes; add Fmoc-Ser(tbu)-OH, NMM, reaction time is 0.5 hours; step (3) add to the peptide chain resin with full side chain protection Peptide cleavage reagent, react for 2.5 hours. The rest is the same as in Example 1.
Example Embodiment
[0108] Example 3
[0109] Step (1) AM PEGMatrix resin reacts with Fmoc-Rink Amide linker and TBTU for 2 hours, then add acetic anhydride: pyridine: DMF mixed solution to react for 2 hours, PEGMatrix resin substitution degree is 0.5mmol / g; step (2) Fmoc -Rink Amide AM PEGMatrix resin, add deprotection reagent, react for 60 minutes; add Fmoc-Ser(tbu)-OH, NMM, reaction time is 2 hours; step (3) add to the peptide chain resin with full side chain protection Cleavage reagent, react for 3 hours. The rest is the same as in Example 1.
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