2,4-Dichlorobenzylamine → 3-Quinolinecarboxamide,8-chloro-1-cyclopropyl-n-[(2,4-dichlorophenyl)methyl]-6,7-difluoro-1,4-dihydro-4-oxo-

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Reaction Steps

15.0 g of 8-chloro-1-cyclopropyl-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (for preparation see DE 3420743 or Y. Kimura et al. J. Med. Chem. 1994, 37 (20), 3344) are dissolved in 500 ml of DMF, and 31.3 g of PyBOP and 10.6 g of 2,4-dichlorobenzylamine are added. After one day the solvent is removed on a rotary evaporator and the residue is purified by flash chromatography on silica gel (toluene/ethyl acetate 95:5). 21.2 g (93% of theory) of the title compound are obtained.

Provenance & Evidence