Synthesis method and application of HWTX-I
A synthetic method, the technology of Huwen, which is applied in the field of synthesis of Huwen analgesic peptide, can solve the problem of few chemical synthesis methods, achieve the effects of shortening the synthesis cycle, improving the purity and stabilizing the process
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[0026] see figure 1 , the invention provides a synthetic method of Huwen analgesic peptide. This synthetic method comprises the following steps:
[0027] Step S01. Provide peptide fragment 1, peptide fragment 2 and peptide fragment 3;
[0028] Wherein, peptide fragment 1 is the 1-8 amino acid and carrier in the main chain sequence of Huwen analgesic peptide;
[0029] Peptide fragment 2 is the 9th-23rd amino acid and carrier in the main chain sequence of Huwen analgesic peptide;
[0030] Peptide fragment 3 is the 24th-33rd amino acid in the main chain sequence of the Huwen analgesic peptide and the carrier; step S02. Use the reaction solution to remove the protective group of the peptide fragment 2, and use the lysate to remove the peptide fragment 2 from the carrier Cleavage to obtain the fully protected peptide fragment 2', and the protecting groups of the 9th and 22nd cysteine amino acids in the fully protected peptide fragment 2' are removed;
[0031] Step S03. Oxidiz...
Embodiment 1
[0074] A synthetic method of Huwen analgesic peptide, its synthetic route please refer to figure 1 , including the following steps:
[0075] S11. Take 500g (0.35mol) of 2-chloro-trityl resin with a degree of substitution of 0.7mmol / g, place it in a polypeptide synthesis reactor, add 4L DCM to it, and make the 2-chloro-trityl resin Swelling occurred and the swollen 2-chloro-trityl resin was washed with DCM.
[0076] 87.2g Fmoc-Gly-OH (0.28mol) and 91.4mL DIEA (0.52mol) were dissolved in DCM, added to the above reactor, reacted for 2h, drained, and washed once with DCM. Add DCM and methanol solution with a volume ratio of 10:1, and stir to seal for 30 minutes. Drain the solvent, wash 3 times with DCM, shrink the resin 3 times with methanol, and obtain Fmoc-Ala-2-chloro-trityl resin after vacuum drying. After monitoring, the substitution degree of the resin is 0.42mmol / g.
[0077] Get 565g Fmoc-Ala-2-chloro-trityl resin, remove the Fmoc protecting group with the DMF solution o...
Embodiment 2
[0103] A synthetic method of Huwen analgesic peptide, its synthetic route please refer to figure 1 , including the following steps:
[0104] S21. Take 500g (0.35mol) of 2-chloro-trityl resin with a degree of substitution of 0.7mmol / g, place it in a polypeptide synthesis reactor, add 4L DCM to it, and make the 2-chloro-trityl resin Swelling occurred and the swollen 2-chloro-trityl resin was washed with DCM.
[0105] Dissolve 87.2g of Fmoc-Gly-OH (0.28mol) and 91.4mL of DIEA (0.52mol) in DCM, add to the above-mentioned reactor, react for 2h, drain and wash once with DCM. Add DCM and methanol solution with a volume ratio of 10:1, and stir to seal for 30 minutes. Drain the solvent, wash with DCM 3 times, shrink the resin 3 times with methanol, and obtain Fmoc-Ala-2-chloro-trityl resin after vacuum drying. After monitoring, the resin substitution degree is 0.29mmol / g.
[0106] Get 565g Fmoc-Ala-2-chloro-trityl resin, remove the Fmoc protecting group with the DMF solution of 20% ...
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