5-Amino-2-chloro-4-fluorophenol → 4-(4-Chloro-2-fluoro-5-hydroxyanilino)-6-methoxy-7-(3-morpholinopropoxy)quinoline hydrochloride hydrate

Participants

Reaction Steps

A solution of 4-chloro-6-methoxy-7-(3-morpholinopropoxy)quinoline hydrochloride (300 mg, 0.73 mmol), and 4-chloro-2-fluoro-5-hydroxyaniline (130 mg, 0.8 mmol), (as described in EP 61741 A2), in 2-pentanol (15 ml) was heated at reflux for 5 hours. The resulting solid was collected by filtration, washed with acetone and dried under vacuum to give 4-(4-chloro-2-fluoro-5-hydroxyanilino)-6-methoxy-7-(3-morpholinopropoxy)quinoline hydrochloride hydrate (283 mg, 73%) as a yellow solid.

Provenance & Evidence