Allyl alcohol derivative and application thereof in protein modification

The invention provides an allyl alcohol derivative and application thereof in preparation of a drug conjugate for site-specific modification of protein or polypeptide N terminal. According to the invention, a complex formed by a metal palladium compound and a phosphine ligand is used as a catalyst,...

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Hauptverfasser: LIN ZENG, LIU BO, WANG YONGQIN, LIU CHAOXI, HUANG WEI, LU MENGRU, LUO CAILI
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creator LIN ZENG
LIU BO
WANG YONGQIN
LIU CHAOXI
HUANG WEI
LU MENGRU
LUO CAILI
description The invention provides an allyl alcohol derivative and application thereof in preparation of a drug conjugate for site-specific modification of protein or polypeptide N terminal. According to the invention, a complex formed by a metal palladium compound and a phosphine ligand is used as a catalyst, and an allyl alcohol derivative is used as an allyl palladium precursor to modify the N-terminal of polypeptide and protein, so that the novel polypeptide or protein N-terminal conjugate is prepared. The method is mild in condition, wide in applicability, high in efficiency and good in selectivity. According to the method, a biological orthogonal group can be introduced into the N-terminal of the antibody, and the antibody drug conjugate is prepared by utilizing a biological orthogonal reaction, or the antibody drug conjugate is prepared by utilizing an allyl alcohol derivative containing a drug structure in one step. 本发明提供了烯丙醇衍生物及其在制备定点修饰蛋白或多肽N端的药物偶联物中的应用。本发明利用金属钯化合物与膦配体形成的配合物为催化剂,以烯丙醇衍生物为烯丙基钯前体实现对多肽、蛋白N端的修饰,制备得到新
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
title Allyl alcohol derivative and application thereof in protein modification
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