反应详情

N-(4-aminophenyl)isoindoline-2-carboxamide (0.0585 g, 0.231 mmol) was suspended in dichloromethane (2 ml) followed by addition of triisopropylethylamine (0.081 ml, 0.462 mmol). (3-Methoxyphenyl)methanesulfonyl chloride (0.061 g, 0.277 mmol) was dissolved in 1 ml dichloromethane and added to the mixture via syringe slowly. The mixture was quenched with water and the separated aqueous layer was extracted with dichloromethane. The combined organic layers were dried over magnesium sulfate, filtered and concentrated. Reverse-phase HPLC provided the title compound. 1H NMR (300 MHz, DMSO-d6) δ ppm 8.65 (s, 1H), 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.34 (t, J=5.6 Hz, 1H), 7.80-7.73 (m, 2H), 7.69-7.61 (m, 2H), 7.44 (d, J=5.0 Hz, 1H), 4.86-4.79 (m, 4H), 3.20 (t, J=6.2 Hz, 2H), 2.46-2.25 (m, 3H), 2.20 (d, J=7.9 Hz, 3H), 2.06-1.78 (m, 1H), 1.52-1.37 (m, 1H); MS (ESI(+)) m/e 438 (M+H)+.

1. additionadded to the mixture via syringe slowly
2. customThe mixture was quenched with water
3. extractionthe separated aqueous layer was extracted with dichloromethane
4. dry with materialThe combined organic layers were dried over magnesium sulfate
5. filtrationfiltered
6. concentrationconcentrated