New method for solid-phase synthesis of side-chain-protected peptide chain

Abstract

The invention relates to a new method for solid-phase synthesis of side-chain-protected peptide chain, which belongs to the technical fields of solid synthesis and preparation of organic compounds and polypeptides. During the peptide chain synthesis, in order to obtain large peptide chain segments, the peptide chain segments protected by the side chains are spliced in liquid phase. When the common polypeptide solid phase synthesis resin is subjected to peptide chain synthesis, the peptide chains are cut off from the resin by acid cracking reagent, side chain protecting groups of the peptide chains are simultaneously released, and then unprotected peptide chains are obtained. A handle is connected with the resin to improve the resin, the peptide chain synthesis is carried out on the 'handle', the peptide chains are cut off from the 'handle' under weak alkaline condition, and the side chain protecting groups can not be released, therefore, the invention can be used for the solid synthesis of side-chain-protected peptide chain.

Description

[0001] The present invention is a new method for solid-phase synthesis of side chains to protect peptide chains, which involves the connection of a "handle" and polypeptide solid-phase synthetic resin, the connection of peptide chains and "handles", and the cutting method of peptide chains from the resin. Through the improvement of the resin with a "handle", the peptide chain can be synthesized on the "handle", and the peptide chain can be cut from the resin with weak alkaline conditions to obtain the peptide chain fragment protected by the side chain. technical field [0002] The invention belongs to the technical field of solid-phase synthesis and preparation of organic compounds and polypeptides. Background technique [0003] Commonly used peptide chain solid-phase synthetic resins include Merrifield resin, Wang resin and Rink Amide resin. When using these resins for peptide chain synthesis, after the peptide chains have been linked, an acidic cleavage reagent is used to ...

AI Technical Summary

Problems solved by technology

However, in the actual synthesis of large peptide chains, two peptide chains are usually used for splicing in the liquid phase. At this time, the side chains of the peptide chains need to be protected, and it is difficult to obtain protected peptide chains using existing resins.

People have developed some resins with special structures, such as HMPA-AM resin, which can cut off the polypeptide chain from the resin under alkaline conditions, without removing the side chain protecting group, and obtain the peptide chain protected by the side chain, but this This kind of resin is expensive, and the high price limits the mass application of this kind of resin

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