5-Amino-2-chloro-4-fluorophenol → 7-Benzyloxy-4-(4-chloro-2-fluoro-5-hydroxyanilino)-6-methoxyquinoline hydrochloride

Participants

Reaction Steps

Using an analogous procedure to that described for the synthesis of Example 11, 7-benzyloxy-4-chloro-6-methoxyquinoline hydrochloride (336 mg, 1 mmol), (prepared as described for the starting material in Example 3), was reacted with 4-chloro-2-fluoro-5-hydroxyaniline (178 mg, 1.1 mmol), (as described in EP 61741 A2), in 2-butanol (15 ml) to give 7-benzyloxy-4-(4-chloro-2-fluoro-5-hydroxyanilino)-6-methoxyquinoline hydrochloride (200 mg, 43%).

Provenance & Evidence