Technology for solid phase synthesis of peptide by WANG strategy

A strategy and technology of synthesis method, applied in the production process field of bulk preparation of raw materials, can solve the problems of poor purity of crude products, increase the difficulty of purification, etc., and achieve the effects of reducing production cost, improving production feasibility, and improving purity

Inactive Publication Date: 2009-06-24
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is the inevitable result of the above two classic methods of peptide synthesis. The purity

Method used

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  • Technology for solid phase synthesis of peptide by WANG strategy
  • Technology for solid phase synthesis of peptide by WANG strategy
  • Technology for solid phase synthesis of peptide by WANG strategy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0037] 1. Synthesis of TP5 Acylethylamide H-Arg-Lys-Asp-Val-Tyr-NHeT (1)

[0038] ①Boc-Tyr-OCH 2 - Preparation of polystyrene resin

[0039] Weigh 10g (10mmol) of chloromethyl (also known as Merrifield) resin (substitution equivalent 1mmol / g, particle size 100-200 mesh, cross-linking degree 1%), and three times the number of moles of Boc-Tyr-OH.K 2 CO 3 and 1 / 10 mole of KI were blended in 150mL DMF. The suspension was rotated and reacted on a hot bath at 60° C. for 25 h, and the reaction suspension was transferred to a No. G2 sand plate filter tube. Use DMF at about 60°C for diafiltration 5 times, about 50 mL each time. This was followed by diafiltration with the following solvents (× times): 95% EtOH × 3, DMF × 3, 50% EtOH / H 2 O×3, DMF×3, absolute ethanol×3. After fully drying, take out the resin and place it under an infrared lamp at about 50°C, and air-dry it to constant weight. It weighs 12.33g, and the weight gain is 2.33g (theoretical weight gain should be 2.44

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Abstract

The invention relates to solid phase synthetic peptide technology by a WANG strategy, in particular to the synthetic mode taking six active oligopeptide as the target structure and adopting cross-matching of Boc-amino acid/strong acid-cleavage resin and Fmoc-amino acid/weak acid-cleavage resin, WANG (without acid-cleavage and nice gain) strategy for short, is adopted; finally the product with satisfactory yield and more lower cost is obtained.

Description

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Claims

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Application Information

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Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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