Diethyl (ethoxymethylene)malonate → HCID 178469649, compound

Participants

Reaction Conditions

Reaction Steps

A neat mixture of 3.58 g of compound of 4-(benzylsulfanyl)-2-fluoroaniline and 3.48 g of diethyl ethoxymethylenemalonate is heated at 135° C. under a slow argon sweep for 1 h, then diluted with 25 mL of diphenyl ether and heated to 260° C., with maintenance of the argon sweep, and kept at that temperature for 90 min. The mixture is then cooled to ca 100° C. and added to 300 mL of stirred heptane. The precipitate is filtered, washed with heptane, and dried in vacuo to provide 4.01 g of ethyl 6-(benzylsulfanyl)-8-fluoro-4-hydroxy-3-quinolinecarboxylate as a yellow solid.

Provenance & Evidence