Univerzita Pardubice Fakulta chemicko- technologická

Univerzita Pardubice

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Novel synthetic approach for kinase inhibitors containing (Z)-3-[amino(phenyl)methylidene]-1,3-dihydro-2H-indol-2-one structure moiety

Autoři: Marek Lukáš | Hanusek Jiří

Rok: 2021

Druh publikace: ostatní - přednáška nebo poster

Strana od-do: nestránkováno

Tituly:

Jazyk	Název	Abstrakt	Klíčová slova
eng	Novel synthetic approach for kinase inhibitors containing (Z)-3-[amino(phenyl)methylidene]-1,3-dihydro-2H-indol-2-one structure moiety	Compounds containing 3-[phenylamino(phenyl)methylidene]indol-2-one (1) structure moiety are established in the treatment of several autoimmune diseases and diverse malignancies. In our group, we recently proved that the thiophile-free Eschenmoser reaction (d0 + a2) of 3-bromoindol-2-ones with various thioamides respresents a versatile synthetic approach for preparation of 3-[amino(phenyl)methylidene]indol-2-ones. In this work, we would like to further demonstrate the usefulness of our synthetic approach for the preparation of known kinase inhibitors (1a-f), especially Nintedanib and Hesperadin. Reaction of several subst. 3-bromoindol-2-ones (2a-f) and thiobenzanilide derivatives (3a-b) was carried out in polar aprotic solvents under mild reaction conditions. Desired compounds were obtained in good to excellent yields (76 – 97 %).	kinase inhibitors; 2H-indol-2-ones; Eschenmoser reaction; thiomides; 3-bromoindol-2-ones