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Solid-phase synthesis method of thymalfasin

A thymosin and solid-phase synthesis technology, which is applied to the preparation methods of thymosin and peptides, chemical instruments and methods, etc., can solve the problems of inability to obtain high-purity products, impurity and product polarity, and high cost, and is conducive to labor. The effect of protection, impurity reduction, and simple steps

Inactive Publication Date: 2014-07-16
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the existence of difficult sequences (sequences with a length of about 6-16 amino acids in the peptide chain from the C-terminus), these methods have low yields, high costs, and impurity and product polarity are too close to obtain high yields. Purity products etc.

Method used

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  • Solid-phase synthesis method of thymalfasin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] 1) Synthesis of Fmoc-Asn(Trt)-Wang resin

[0052] Weigh 10g Wang resin with a degree of substitution of 0.4mmol / g and swell it with 100ml DMF for 2 hours, then drain it, add 100ml DMF solution containing Fmoc-Asn(Trt)-OH7.2g, DIC1.9ml, HOBT1.7g, DMAP0.3g, room temperature After reacting for 3 hours, the reaction solution was drained, and the resin was washed three times with 100 ml DMF respectively to obtain Fmoc-Asn(Trt)-King resin.

[0053] 2) Coupling

[0054] The Fmoc-Asn(Trt)-WangResin obtained in step 1) was deprotected by Fmoc twice with 100ml 20% piperidine / DMF solution respectively, then the resin was washed 6 times with 100ml DMF respectively, and then Fmoc-Glu(OtBu)-OH5. 1g and 100ml of DMF reaction solution containing 1.9ml of DIC and 1.7g of HOBT were reacted at 28°C, and the color reaction of ninhydrin was used as the basis for judging the end point of the reaction. After the reaction, the reaction solution was drained, and the resin was washed with DMF ...

Embodiment 2

[0061] 1) Synthesis of Fmoc-Asn(Trt)-Wang resin

[0062] Weigh 10g Wang resin with a degree of substitution of 0.4mmol / g and swell it with 100ml DMF for 2 hours, then drain it, add 100ml DMF solution containing Fmoc-Asn(Trt)-OH7.2g, DIC1.9ml, HOBT1.7g, DMAP0.3g, room temperature After reacting for 3 hours, the reaction solution was drained, and the resin was washed three times with 100 ml DMF respectively to obtain Fmoc-Asn(Trt)-King resin.

[0063] 2) Coupling

[0064] The Fmoc-Asn(Trt)-WangResin obtained in step 1) was de-Fmoc-protected twice with 100ml 20% piperidine / DMF solution respectively, then the resin was washed 6 times with 100ml DMF respectively, and then Fmoc-Glu(OtBu)-OH5. 1g and 100ml of DMF reaction solution containing 1.9ml of DIC and 1.7g of HOBT were reacted at 28°C, and the color reaction of ninhydrin was used as the basis for judging the end point of the reaction. After the reaction, the reaction solution was drained, and the resin was washed with DMF fo...

Embodiment 3

[0071] 1) Synthesis of Fmoc-Asn(Trt)-Wang resin

[0072] Weigh 10g Wang resin with a degree of substitution of 0.5mmol / g and swell it with 100ml DMF for 2 hours, then drain it, add 100ml DMF solution containing Fmoc-Asn(Trt)-OH9.0g, DIC2.3ml, HOBT2.0g, DMAP0.4g, room temperature After reacting for 3 hours, the reaction solution was drained, and the resin was washed three times with 100 ml DMF respectively to obtain Fmoc-Asn(Trt)-King resin.

[0073] 2) Coupling

[0074] The Fmoc-Asn(Trt)-WangResin obtained in step 1) was de-Fmoc-protected twice with 100ml20% piperidine / DMF solution respectively, and then the resin was washed 6 times with 100mlDMF respectively, and then Fmoc-Glu(OtBu)-OH6. 4g and 100ml of DMF reaction solution containing 2.3ml of DIC and 2.0g of HOBT were reacted at 28°C, and the color reaction of ninhydrin was used as the basis for judging the end point of the reaction. After the reaction, the reaction solution was drained, and the resin was washed with DMF ...

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Abstract

The invention relates to a solid-phase synthesis method of thymalfasin. The solid-phase synthesis method comprises the process steps: solid-phase linear synthesis of linear thymalfasin is carried out, a DMF solution of a salt composed of bulky anions and monovalence cations is used as a reaction solvent in a difficult sequence, hydrogen bond formation is interfered, and a beta structure of a peptide chain is destroyed. The process can overcome the polypeptide synthesized difficult sequence, improves the coupling rate of the difficult sequence so as to improve the yield of thymalfasin, reduces the production cost, and is beneficial for industrialized production.

Description

technical field [0001] The invention relates to the field of polypeptide synthesis, in particular to a new solid phase synthesis method of the thymus method. Background technique [0002] Thymus Faxin was once called thymosin α1 thymosin α1, which was first isolated from thymosin component 5 by Goldstein in 1977 and confirmed that its primary structure consists of 28 amino acids, N-terminal acetylation, molecular mass 3108Da, isoelectric point 4.2. Thymusfasin is a new type of immunoregulatory factor, it induces the transformation of stem cells into mature T lymphocytes, stimulates the lymphatic system, and improves the immune function of the body. Clinically, thymusfasin is used to improve the immune function of T cells, treat viral hepatitis and delay The occurrence and development of certain geriatric diseases. Thymus fasin also has anti-infection, anti-virus and anti-tumor effects, especially for cancer immunotherapy. [0003] Thymus Faxin was developed and launched b...

Claims

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Application Information

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IPC IPC(8): C07K14/575C07K1/06C07K1/04
CPCY02P20/55C07K14/57581
Inventor 赵志全李铁健颜凯
Owner SHANDONG NEWTIME PHARMA
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