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Preparation method of synthesizing growth chalone from solid phase polypeptide
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A solid-phase peptide synthesis, somatostatin technology, applied in the fields of peptide preparation, somatostatin, chemical instruments and methods, etc., can solve the problems of low column efficiency, environmental pollution, cost increase and so on
Inactive Publication Date: 2007-03-07
SHANGHAI SOHO YIMING PHARMA +1
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A notable defect in this patent is that it is purified in the form of trifluoroacetate, which pollutes the environment; the intermediate product is oxidatively cyclized in hydrogenperoxide or dimethyl sulfoxideaqueous solution, and the pollution of the three wastes is serious; using C#-[18] Bonded silica gel medium-pressure column for purification, because the medium-pressure column has low column efficiency and time-consuming, the purification yield is low and the cost is greatly increased
Therefore, current methods limit the large-scale production and use of somatostatin
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Embodiment 1
[0117] In the example:
[0118] Said peptide-connecting reagent is: NMM:DMF=1:10, volume ratio;
[0122] Weigh 50g of trityl resin (100-400 mesh, 1.0mmol / g), soak in 500ml of DMF for 30 minutes to fully swell the resin, add 44ml of DIPEA, 87.9g of Fmoc-Cys(Trt)-OH, and react at 25°C 1 hour. Add 20 ml of methanol and react at 25°C for 1 hour. Blow dry with nitrogen, wash the resin three times with DMF, and blow dry with nitrogen.
[0123] (2) Preparation of Fmoc-Ser(tBu)-Cys(Trt)-resin:
[0124] In the Fmoc-Cys(Trt)-resin of step (1), add 500ml of decappingreagent, react for 30 minutes at 25°C, blow dry, wash with DMF, blow dry, add Fmoc-Ser(tBu )-OH 57.5g, TBTU 48.1g and HOBT 20.2g mixture, reacted at 25°C for 2 hours, dried, washed with DMF and ethanol respectively, and dried to obtain Fmoc-Ser(tBu)-Cys(Trt)-resin;...
Embodiment 2
[0162] Adopt the same method and processing condition as embodiment 1, wherein:
[0163] Use 4-methoxytrityl resin as the starting material, connect Fmoc-Cys(Trt)-OH with the same method as before, then add decapping reagent, react at 25°C for 0.5 hours, add Fmoc dissolved in peptide reagent -The mixture of amino acid, TBTU / HBTU and HOBT was reacted at 25°C for 2 hours, and then subjected to reactions such as peptide cutting and oxidation to obtain 14.8g of white loose block finished product.
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Abstract
The invention discloses a chalone preparing method of solid-phase polypeptide, which comprises the following steps: adopting 2-chloride-trityl resin, 4-methyl trityl resin or 4-methoxyl trityl resin as raw material; connecting amino acid with protective group according to solid-phase synthetic method; obtaining protected octapeptide resin; removing Fmoc-protective group sequently; stripping side-chain protective group; cuttingpeptide to obtain reduced aoqu-peptide; oxidizing through air under pH 7-11 condition; separating and purifying rought product through C18 (C8) column to produce exquisite.
Description
technical field [0001] The invention relates to a preparation method of somatostatin, in particular to a preparation method of solid-phase polypeptide synthesis of somatostatin. Background technique [0002] Chinese name: somatostatin. Other names: somatostatin-releasing inhibitory hormone, trade name: stanine. English name: Somatostatin, Stilamin. [0003] Structural formula: [0004] [0005] Molecular formula and molecular weight: C 76 h 104 N 18 o 19 S 2 , 1637.9. [0006] Clinical use: severe acute esophageal variceal rupture and bleeding, severe acute gastric and duodenal ulcer bleeding, acute erosive gastritis or hemorrhagic gastritis, adjuvant treatment of pancreas, gallbladder and intestines, adjuvant treatment of diabetic ketoacidosis. [0007] Adverse reactions: nausea, dizziness, facial flushing in a few cases. Nausea and vomiting may occur when the injection rate is higher than 50 μg per minute. [0008] Somatostatin is synthesized by the median em...
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