反应详情

温度

120 °C

A mixture of trans 4-methanesulfonyl-cyclohexylamine trifluoroacetic acid salt (383 mg, 1.32 mmol), 1-benzenesulfonyl-4-chloro-5-nitro-1H-pyrrolo[2,3-b]pyridine (536 mg, 1.60 mmol), diisopropylethylamine (0.69 mL, 4.0 mmol) in propan-2-ol (5.5 mL), were heated at 120° C. for 10 minutes using microwave irradiation. The mixture was cooled to 0° C. and filtered, the resulting solid washed with propan-2-ol and ether, then dried under vacuum to give 588 mg (93%) of trans (1-benzenesulfonyl-5-nitro-1H-pyrrolo[2,3-b]pyridin-4-yl)-(4-methanesulfonyl-cyclohexyl)-amine as a bright yellow solid. 1H NMR (400 MHz, CDCl3) δ: 9.11 (s, 1H), 8.99 (d, 1H), 8.20 (m, 2H), 7.64 (m, 2H), 7.53 (t, 2H), 6.66 (d, 1H), 3.95 (ddd, 1H), 2.95 (m, 1H), 2.91 (s, 3H), 2.40 (m, 4H), 1.85 (m, 2H), 1.52 (m, 2H).

1. custommicrowave irradiation
2. temperatureThe mixture was cooled to 0° C.
3. filtrationfiltered
4. washthe resulting solid washed with propan-2-ol and ether
5. customdried under vacuum