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Synthesis and preparation process of rgd cyclic peptide

A preparation process and cyclic peptide technology, applied in the field of solid-phase peptide synthesis, can solve the problems of complexity, trouble, and low crude product yield, and achieve the effects of high product yield, reasonable process and simple operation.

Active Publication Date: 2016-08-17
苏州强耀生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method is relatively complicated, and there is an additional step of full protection cleavage and condensation cyclization in the liquid phase, and the late precipitation step of the cyclic peptide in the solution is relatively troublesome, and the yield of the crude product is not high.

Method used

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  • Synthesis and preparation process of rgd cyclic peptide

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Synthetic peptide sequence cyclo(RGDfK):

[0019] The cyclic peptides are formed by amide bonds at the beginning and end. Select the company's semi-automatic peptide synthesizer, weigh an appropriate amount of 2-chlorotrityl chloride resin into the reaction glass column, add an appropriate amount of DMF to soak and swell, weigh an appropriate amount of FMOC-Asp(oall)-OH protected amino acid and add it to the resin , add an appropriate amount of DMF solvent as the reaction solution, blow nitrogen to dissolve the amino acid, add an appropriate amount of DIEA catalyst, react at room temperature for 1 hour, then add a small amount of methanol solvent to react for 20 minutes to seal off the reactive sites on the resin. The resin was repeatedly washed with DMF and methanol solvents and the solvent was aspirated so that the first amino acid, aspartic acid, was attached to the resin. An appropriate amount of piperidine solvent was added to react for 15 minutes to remove the am...

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Abstract

The invention discloses a synthesis and preparation process of RGD cyclic peptide in the field of solid-phase polypeptide synthesis. The new method is to use 2-chlorotrityl chloride resin as the carrier, connect the first D-aspartic acid amino acid with a special protective group on the carboxyl group of the side chain, and then connect the linear peptide of the RGD sequence peptide on the On the resin, after the last amino acid is connected, piperidine is not used to remove the protective group FMOC of the amino group, and a special catalyst is added to remove the carboxyl group of the first D-aspartic acid side chain directly on the resin, and then piperidine is added. The amino protecting group FMOC of the terminal amino acid is removed by pyridine, and then a condensing agent is added to directly dehydrate and condense the exposed carboxyl and amino groups at the head and end of the linear peptide on the resin to form a cyclic peptide in the form of an amide bond. Finally, the cyclic peptide is directly cut from the resin with a cutting solution. The invention has the advantages of advanced technology, simple operation, high product yield, improved synthesis efficiency and the like.

Description

technical field [0001] The invention relates to a synthesis and preparation process of RGD cyclic peptide in the field of solid-phase polypeptide synthesis. Background technique [0002] Cyclic peptides refer to compounds formed by amino acid peptide bonds, and are divided into cyclic peptides and linear peptides according to whether they are cyclic or not. Cyclic peptide compounds have various biological activities, including anti-tumor, anti-HIV, anti-bacterial, anti-malarial, sleeping, inhibition of platelet aggregation, antihypertensive, inhibition of tyrosinase, inhibition of cyclooxygenase, inhibition of lipid peroxidase , estrogen-like, immunosuppressive and other biological activities. Using 2-chlorotrityl chloride resin as a carrier, synthesize small molecular polypeptides with R arginine, G glycine, D aspartic acid and other amino acids on the resin, and use the side chain of D aspartic acid The carboxyl group and the terminal amino group of the last amino acid i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/12C07K1/06C07K1/04C07K1/14
CPCY02P20/55
Inventor 王锡平
Owner 苏州强耀生物科技有限公司
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