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filingDate 2021-06-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2023-01-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2023-01-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-113527121-B
titleOfInvention A construction method of C(sp3)-C(sp2) bond and preparation method of β-aryl amino acid
abstract The invention provides a method for constructing a C (sp3) -C (sp2) bond and a method for preparing a β-aryl amino acid, and relates to the technical field of chemical substance synthesis and transition metal application, including combining amino acid β-C (sp3) with phenol The ring carbon C (sp2) where the hydroxyl group is located is directly coupled to construct a C-C bond. In this process, the amino acid containing inactive β-C (sp3) -H and the ligand L 1 of specific structure are complexed with divalent nickel to form a four-coordinated chelate, and then combined with sulfonic acid phenol under alkaline conditions Under the catalysis of palladium, the ester completes amino acid inactive β‑C (sp3) ‑H arylation and proton transfer reactions, realizes the construction of C (sp3) ‑C (sp2) bond, and finally releases β‑C arylation by hydrolysis Amino Acids and Ligand L 1 . The method for constructing the C (sp3) -C (sp2) bond provided by the invention has the advantages of simple and convenient operation, low cost, strong reaction versatility, and high yield and stereoselectivity. The synthesis method of the present invention provides a new method for preparing various types of unnatural β-aryl amino acids, amino acid/peptide modification of biologically active phenolic compounds, and provides a new method for the design and synthesis of new drugs. new ways and options.
priorityDate 2021-06-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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