Preparation method for synthesizing anti-inflammatory decapeptide by using solid-phase polypeptide

A solid-phase peptide synthesis, anti-inflammatory decapeptide technology, applied in the preparation methods of peptides, chemical instruments and methods, peptides and other directions, can solve problems such as difficulties in peptide synthesis, and achieve the effects of stable process, stable quality and short production cycle

Active Publication Date: 2014-10-08
SHANGHAI SOHO YIMING PHARMA
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are another 6 D-Nle, so it brings ce

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method for synthesizing anti-inflammatory decapeptide by using solid-phase polypeptide

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0078] Example 1

[0079] The examples and the list of raw materials used in the foregoing process are as follows:

[0080] No Name manufacturer 1 Rink Amide MBHA resin Tianjin Hecheng Technology Co., Ltd. 2 Fmoc-D-Tyr(tBu)-OH Suzhou Tianma Pharmaceutical Group 3 Fmoc-D-Arg(Pbf)-OH Suzhou Tianma Pharmaceutical Group 4 Fmoc-Gly-OH Suzhou Tianma Pharmaceutical Group 5 Fmoc-D-Nle-OH Suzhou Tianma Pharmaceutical Group 6 Boc-D-Arg-OH Suzhou Tianma Pharmaceutical Group 7 1-hydroxy-7-azobenzotriazole (HOAt) Suzhou Tianma Pharmaceutical Group 8 Benzotriazole-N,N,N',N'-tetramethylurea hexafluorophosphate (HBTU) Suzhou Tianma Pharmaceutical Group 9 N,N-Diisopropylethylamine (DIPEA) Sinopharm Chemical Reagent Co., Ltd. 10 Dimethylformamide (DMF) Sinopharm Chemical Reagent Co., Ltd. 11 Methanol Sinopharm Chemical Reagent Co., Ltd. 12 Hexahydropyridine (PIP) Sinopharm Chemical Reagent Co., Ltd. 13Mercaptoethanol (HOCH 2 CH 2 SH) Sinopharm Chemical Reagent Co., Ltd. 14 Triisopropylsilane (TI...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention discloses a preparation method for synthesizing anti-inflammatory decapeptide by using solid-phase polypeptide. The preparation method comprises the following steps: by taking RinkAmideMBHA resin as a starting raw material, sequentially connecting D-amino acid with protecting groups by using a solid-phase synthesis method, to obtain protective decapeptide resin, sequentially removing Fmoc-protecting groups, and conducting TFA cleaving to obtain a crude product, conducting separation and purification on the crude product through a C18 column, carrying out freeze drying to obtain the anti-inflammatory decapeptide. The method is stable in technology, convenient in sources of raw materials and auxiliaries, short in production period, high in yield, stable in quality, low in production cost, high in peptide grafting yield, capable of avoiding the use of high-toxicity reagents such as hydrogen fluoride and less in three-waste pollution. The peptide grafting yield in each step can achieve more than 98.5%; the peptide cleaving yield is 98.3%, the total yield is 47.9%, and the purity of the HPLC-determined product is 99.65%.

Description

technical field [0001] The invention relates to a preparation method of anti-inflammatory decapeptide, in particular to a preparation method of solid-phase polypeptide synthesis anti-inflammatory decapeptide. Background technique [0002] Anti-inflammatory decapeptide, English name: Delmitide, molecular formula: C 59 h 105 N 17 o 11 ; CAS registration number: 287096-87-1; Molecular weight: 1227.8; Carbon, hydrogen, nitrogen ratio: C: 57.68%, H: 8.61%, N: 19.38%. Amino acid sequence: D-Arg-D-Nle-D-Nle-D-Nle-D-Arg-D-Nle-D-Nle-D-Nle-Gly-D-Tyr-NH 2 ; [0003] Structural formula: [0004] [0005] Anti-inflammatory decapeptide is a synthetic 10-peptide used in the treatment of ulcerative colitis (IBD). With the continuous improvement of people's living standards, ulcerative colitis (IBD) is the main disease of inflammatory bowel disease and has become a common disease that endangers human health. At present, there is no specific chemotherapeutic drug for the treatment o...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07K7/06C07K1/14C07K1/06C07K1/04
CPCY02P20/55
Inventor 王文琪刘湘艳崔颀周逸明
Owner SHANGHAI SOHO YIMING PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products