反应详情

The reaction mixture of 3-(2-methoxyphenyl)-5-methylisoxazole-4-carboxylic acid (0.131 g, 0.561 mmol), 2,4-dichloro-5-(piperazin-1-yl)aniline, 2 TFA (0.253 g, 0.534 mmol), EDC (0.123 g, 0.641 mmol) and DMAP (0.130 g, 1.07 mmol) in DCM (4 mL) was stirred at RT overnight. The crude product was purified by flash chromatography (MeOH/DCM, gradient 2%-4%, Rf 0.31 with 3% MeOH) to give 0.221 g of the title compound (90% yield). 1H-NMR (CD3OD, 400 MHz): δ 7.57-7.50 (2H, m), 7.19 (1H, s), 7.18-7.07 (2H, m), 6.43 (1H, s), 3.81 (3H, s), 3.74 (2H, s), 3.24 (2H, s), 2.88 (2H, s), 2.53 (3H, s), 2.35 (2H, s).

1. customThe crude product was purified by flash chromatography (MeOH/DCM, gradient 2%-4%, Rf 0.31 with 3% MeOH)