5-Amino-2-chloro-4-fluorophenol → 2-Chloro-4-fluoro-5-{[6-methoxy-7-(2-methoxyethoxy)cinnolin-4-yl]amino}phenol

Participants

Reaction Conditions

Reaction Steps

A solution of 4-chloro-6-methoxy-7-(2-methoxyethoxy)cinnoline (0.1 g, 0.74 mmol), (prepared as described for the starting material in Example 2), and 4-chloro-2-fluoro-5-hydroxyaniline (432 mg, 0.82 mmol), (prepared as described in EP 061741 A2), in DMF (2.5 ml) was heated at 140° C. for 45 minutes. The work up procedure was as described in Example 6 and gave 4-(4-chloro-2-fluoro-5-hydroxyanilino)-6-methoxy-7-(2-methoxyethoxy)cinnoline as the hydrochloride salt (yellow solid, 157 mg, 49%).

Provenance & Evidence