反应详情

Heat a mixture of 6-(8-chloropyrido[2,3-b]pyrazin-3-yl)-5-(trifluoromethyl)nicotinamide (70.6 mg, 0.2 mmol) and 2-amino-5-trifluoromethyl-pyrazine (98.4 mg, 0.6 mmol) in a screw cap vial at 140° C. for 20 hours under N2 atmosphere. Purify the reaction mixture by column chromatography using EtOAc to 1% MeOH/EtOAc as eluent to afford the title compound as a pale yellow solid. 1H NMR (400 MHz, CDCl3) δ 11.182 (s, 1H), 9.456 (s, 1H), 9.44(s, 1H), 9.074 (d, 1H, J=1.3 Hz), 9.052 (s, 1H), 8.87(d, 1H, J=1.3 Hz), 8.828 (d, 1H, J=2.6 Hz), 8.542 (s, 1H), 7.974 (1, 1H). MS=481.42 (M+H). The IC50 determined as described in Example 6 is less than 1 micromolar.

1. temperatureHeat
2. customcap vial at 140° C. for 20 hours under N2 atmosphere
3. customPurify the reaction mixture by column chromatography