3,5-Dichloro-2,4-difluorobenzoyl fluoride → ethyl 3-(cyclopropylamino)-2-(3,5-dichloro-2,4-difluorobenzoyl)prop-2-enoate

Participants

Reaction Steps

3,5-Dichloro-2,4-difluoro-benzoyl fluoride is reacted analogously to Example A, the reaction passing through the following stages: ethyl(3,5-dichloro-2,4-difluoro-benzoyl)-acetate (yield: 43%, boiling point 133° C./2.5 mm Hg), ethyl 2-(3,5-dichloro-2,4-difluoro-benzoyl)-3-ethoxy-acrylate (crude yield: 91%, oil), ethyl 2-(3,5-dichloro-2,4-difluoro-benzoyl)-3-cyclopropylamino-acrylate (yield: 96%, melting point 71°-74° C.), ethyl 6,8-dichloro-1-cyclopropyl-7-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate (yield: 97%, melting point 215°-217° C., with decomposition) and 6,8-dichloro-1-cyclopropyl-7-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (yield: 93%; melting point 204°-206° C.).

Provenance & Evidence