Preparation method for uniform cyclic peptide Cyclo-(Cys)6
A technology of cyclic peptide and resin, which is applied in the field of cyclic peptide compound cyclic peptide Cyclo-6 and its synthesis and preparation, to achieve the effect of simple operation, good reactivity and reasonable process
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[0027] Example 1:
[0028] A homocyclic peptide Cyclo-(Cys) 6 preparation methods, including:
[0029]Step 1. Soak the 2-chlorotrityl chloride resin with dichloromethane, and shake for 30min; remove the solvent after the resin is swollen, and take the amino group with a fluorene methoxycarbonyl protecting group and the side chain mercapto group with a trityl protecting group The cysteine of 3-fold molar excess was added to the resin, and N,N-diisopropylethylamine was added to the resin in a ten-fold molar excess, and then DMF was added to dissolve it, and the reaction was shaken at room temperature for 30 minutes; then methanol was added to incubate for 20 minutes; The reactive sites on the resin were blocked; the resin was repeatedly washed with DMF and methanol solvent and the solvent was removed, and the first amino acid was attached to the resin; after the solvent was removed, a lysis solution was added to remove the protective group on the cysteine amino group Fluor...
Example Embodiment
[0033] Example 2:
[0034] A homocyclic peptide Cyclo-(Cys) 6 preparation methods, including:
[0035] Step 1. Soak the 2-chlorotrityl chloride resin with dichloromethane, and shake for 30min; remove the solvent after the resin is swollen, and take the amino group with a fluorene methoxycarbonyl protecting group and the side chain mercapto group with a trityl protecting group The cysteine of 3-fold molar excess was added to the resin, and N,N-diisopropylethylamine was added to the resin in a ten-fold molar excess, and then DMF was added to dissolve it, and the reaction was shaken at room temperature for 30 minutes; then methanol was added to incubate for 20 minutes; Rinse the resin repeatedly with DMF and methanol solvent and remove the solvent, the first amino acid is connected to the resin; after removing the solvent, add the lysate to remove the protecting group fluorenyl methoxycarbonyl on the cysteine amino group; take a few beads of resin , after fully washing with...
Example Embodiment
[0039] Example 3:
[0040] A homocyclic peptide Cyclo-(Cys) 6 preparation methods, including:
[0041] Step 1. Soak the 2-chlorotrityl chloride resin with dichloromethane, and shake for 30min; remove the solvent after the resin is swollen, and take the amino group with a fluorene methoxycarbonyl protecting group and the side chain mercapto group with a trityl protecting group The cysteine of 3-fold molar excess was added to the resin, and N,N-diisopropylethylamine was added to the resin in a ten-fold molar excess, and then DMF was added to dissolve it, and the reaction was shaken at room temperature for 30 minutes; then methanol was added to incubate for 20 minutes; Rinse the resin repeatedly with DMF and methanol solvent and remove the solvent, the first amino acid is connected to the resin; after removing the solvent, add the lysate to remove the protecting group fluorenyl methoxycarbonyl on the cysteine amino group; take a few beads of resin , after fully washing with...
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