Production of acetooxdralpeptide

A technology of octreotide acetate and production process, which is applied in the production of bulk chemicals and peptides, and can solve the problems of price restrictions and high prices for patients

Inactive Publication Date: 2004-04-21
JIANGSU SOHO INTERNATIONAL GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to solve the problem that the existing synthetic octreotide acetate process in the prior art has

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0005] (1) Take 10g of Boc-Thr(Ac)-Wang resin (1.01mmol / g, 1.01mmol) and put it into a reaction vessel, soak it with 100mlDMF, wash to make the resin fully expand, add 50ml of TFA and 50ml of dichloromethane The mixed solution was reacted at 25°C for half an hour, washed three times with DMF, absolute ethanol, dichloromethane, and DMF respectively, drained, added 8ml of triethylamine and 92ml of dichloromethane mixture, reacted at 25°C for ten minutes, and washed with DMF and dichloromethane were washed three times each, drained, added 23.4g Fmoc-Cys(Trt)-OH, 12.8g TBTU, 6.1g HOBt, dissolved with 80ml of peptide reagent, reacted at 25°C for one hour, respectively with DMF, without Wash with water, ethanol, dichloromethane, and DMF three times each, and drain. (2) If the above-mentioned reagents are positive for amino groups by Karl Fischer’s method, use 40ml of peptide-connecting reagent to make up the connection, and then repeat with DMF, absolute ethanol, dichloromethane, and...

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PUM

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Abstract

A process for preparing the octretide acetate includes such steps as loading Boc-Thr(Ac)-Wang resin in reactor, adding the liquid mixture of TFA and dichloromethane, reacting, washing, adding the liquid mixture of triethane and dichloromethane, adding Fmoc-Cys(Trt)-OH, TBTU and HOBt, dissolving in peptide conjugating agent, testing amino radical to show negative, adding end closing agent and cap removing agent, washing, adding Fmoc-Thr(Trt)-OH, TBTU and HOBt, dissolving in peptide conjugating agent, testing amino radical to show negative, adding end closing agent and cap removing agent, washing, adding Fmoc-Thr(tBu)-OH, TBTU, HOBt, Fmoc-Lys(Boc)-OH, TBTU and HOBt, dissolving, adding Fmoc-D-Trp(Boc)-OH, TBTU and HOBt, dissolving in peptide conjugating agent, adding Fmoc-Phe-OH, TBTU and HOBt, washing, dewatering, adding Fmoc-Cys(Trt)-OH, TBTU, HOBt, Fmoc-D-Phe-OH, TBTU and HOBt, drying to obtain octapeptide resin, further processing, and freez drying. Its advantage is low cost.

Description

technical field [0001] The invention relates to a production process of octreotide acetate. Background technique [0002] Octreotide is a synthetic somatostatin, which is the most effective hormone drug in clinical application in the 1990s. It has the same pharmacological effect as natural somatostatin, but its half-life is extended by 30 times. It has a wide range of application values. It can Inhibit the secretion of a variety of gastrointestinal hormones and other endocrine functions, clinically treat various types of pancreatitis, pancreatic fistula, intestinal fistula, liver cirrhosis, esophageal and gastric variceal bleeding, peptic ulcer bleeding, severe diarrhea, etc. And it is expected to be used in the treatment of digestive system endocrine tumors, but the existing synthesis process uses expensive L-Thr(ol), so that the use of patients is limited by the price. Contents of the invention [0003] The purpose of the invention is to solve the problem that the exist...

Claims

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Application Information

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IPC IPC(8): C07K7/64
CPCY02P20/55
Inventor 周逸明
Owner JIANGSU SOHO INTERNATIONAL GROUP CORPORATION
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