反应详情

In a similar fashion using route 19 general procedure 42, 6-methoxyquinolin-8-amine (Intermediate 23) (300 mg, 1.7 mmol), chlorosulfonic acid (120 μl, 1.8 mmol), PCl5 (370 mg, 1.8 mmol), TEA (360 μl, 2.5 mmol), 3-chloro-2-methylaniline (810 μl, 6.8 mmol) and DIPEA (600 μl, 3.4 mmol) gave the title compound (15 mg, 2%) after purification by column chromatography with DCM/n-hexane (1:1) as the eluent, followed by recrystallisation from EtOAc/n-hexane and then further purification by column chromatography with n-hexane/EtOAc (4:1) as the eluent.