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A solid-phase synthesis, peptide hydrazide technology, applied in the field of solid-phase synthesis of peptides, can solve the problem of long aminolysis time and so on
Pending Publication Date: 2021-12-03
SHENZHEN JYMED TECH
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Problems solved by technology
On the one hand, this patented method needs to prepare free ethylamine-THF solution in advance, and on the other hand, the amination time is l
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Embodiment 1
[0023] Example 1 Activation of Wang Resin 1
[0024] Weigh 5.00g of Wang resin (degree of substitution 0.84mmol / g), add 50ml of dichloromethane to soak for 15min to make it fully swell, filter to remove the solvent, add 50ml of dichloromethane again, and place in an ice bath to cool. Add 1.27g triethylamine (3eq), then add 1.25g triphosgene in batches, keep it at low temperature for 30min, move to room temperature and continue the reaction for 2h. After the reaction was completed, the solution was removed by suction filtration, the resin was washed three times with DMF and three times with dichloromethane, and then vacuum-dried to obtain 5.27 g of resin.
Embodiment 2
[0025] Embodiment 2 Activation of Wang Resin 2
[0026] Weigh 5.00g Wang resin (degree of substitution 0.84mmol / g), add 50ml THF and soak for 15min to make it fully swell, filter to remove solvent, add 50ml THF again, add 2.05g carbonyldiimidazole at room temperature, and stir for 2h. After the reaction was completed, the solution was removed by suction filtration, the resin was washed three times with DMF and three times with dichloromethane, and then vacuum-dried to obtain 5.40 g of resin.
Embodiment 3
[0027] Example 3 Activation of Wang Resin 3
[0028] Weigh 5.00g of Wang resin (degree of substitution 0.84mmol / g), add 50ml of dichloromethane to soak for 15min to make it fully swell, filter to remove the solvent, add 50ml of dichloromethane again, and place in an ice bath to cool. Add 1.27g of triethylamine (3eq), then add 2.54g of p-nitrophenyl chloroformate in batches, keep at low temperature for 30min, move to room temperature to continue the reaction for 2h. After the reaction was completed, the solution was removed by suction filtration, the resin was washed three times with DMF and three times with dichloromethane, and then vacuum-dried to obtain 5.69 g of resin.
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Abstract
The invention relates to the field of polypeptide synthesis, in particular to a solid-phase synthesis method of polypeptide. The method comprises the following steps: 1) activating hydroxyl resin into X-CO-O-Resin by an activating agent, wherein X is an activating group; 2) reacting the X-CO-O-Resin with NH2NH2 to synthesize NH2NH-CO-O-Resin, or reacting the X-CO-O-Resin with Fmoc-NHNH2 to synthesize Fmoc-NHNH-CO-O-Resin, and then removing Fmoc to obtain NH2NH-CO-O-Resin; 3) coupling the NH2NH-CO-O-Resin with amino acid or a peptide fragment according to a peptide sequence to obtain peptide hydrazide resin; 4) cracking the peptide hydrazide resin by a cracking reagent to obtain peptide hydrazide; 5) converting the peptide hydrazide into an acyl azide or hydrazine terminal structure which can be used for coupling in water, thereby preparing some polypeptides with special modification at carbon terminals. The method is particularly suitable for relin type polypeptide with ethylamino or semicarbazide at the carbon terminals. The relin polypeptide is prepared by a peptide hydrazide method, so that the cost can be greatly reduced, the operation steps are reduced, and the emission of waste water, waste gas and solid wastes is reduced. The synthesis process is safe and stable, has no adverse side reaction, and is suitable for industrial large-scale production.
Description
technical field [0001] The invention relates to the field of polypeptide synthesis, in particular to a method for solid-phase synthesis of polypeptides. Background technique [0002] There are two main methods for peptide synthesis: solid-phase synthesis and liquid-phase synthesis. Liquid-phase synthesis is mainly used for the synthesis of short peptides, and has the disadvantages of complex intermediate purification operations, cumbersome post-processing operations, and long synthesis cycles. R. Bruce Merrifield first proposed the solid-phase peptide synthesis method (SPPS) in 1963. Its synthesis is convenient, rapid, and the reaction conditions are mild, and it is widely used quickly. At present, more than 85% of peptide drugs are obtained through solid-phase synthesis. The peptide hydrazide peptide coupling method in the solid-phase peptide synthesis method is a new chemoselective peptide coupling method reported by Professor Liu Lei in 2011. This method uses the C-termi...
Claims
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