The invention discloses an arylation or
alkynylation modification method of a natural
amino acid-oriented polypeptide C (sp3)-H bond. The method comprises the following steps of: in the presence of an oxidant, a catalyst, an additive and a
solvent, by taking a compound shown in a formula (III) or a formula (IV) as a modification
raw material, respectively performing arylation or
alkynylation modification of the C (sp3)-H bond on an
alanine side chain in a compound shown in a formula (I) or a formula (II). According to the method disclosed by the invention, a series of
fluorescence-labeled
alanine-containing polypeptide derivatives, side-chain-modified
tyrosine-containing polypeptide derivatives, side-chain-modified
phenylalanine-containing polypeptide derivatives and alkynyl-modified
alanine-containing polypeptide derivatives can be synthesized. The method disclosed by the invention has the advantages that a guide group does not need to be introduced in advance or subsequently removed, the
atom economy and
gait economy are high, the conditions are mild, the substrate applicability range is wide, the method is not influenced by
amino acid configuration, and the like, and is a polypeptide modification method with excellent popularization prospects.