反应详情

Triethylamine (81.3 g, 0.803 mol) was added to a solution of 230.0 g (0.731 mol) of 7-benzyloxy-4-chloro-3-nitroquinoline (230.0 g, 0.731 mmol), prepared in Parts A-D of Example 1, in methanol (1.84 L). Hydroxyisobutylamine (71.6 g, 0.803 mol) was then added over a period of five minutes; the temperature rose from 30° C. to 39° C. during the addition. The reaction mixture was heated at reflux for four hours and then allowed to cool to room temperature. The solid product was isolated by filtration, washed with ethanol (1 L), and dried under vacuum at 55° C. to provide 261.2 g of 1-[(7-benzyloxy-3-nitroquinolin-4-yl)amino]-2-methylpropan-2-ol.

1. additionthe temperature rose from 30° C. to 39° C. during the addition
2. temperatureThe reaction mixture was heated
3. temperatureat reflux for four hours
4. customThe solid product was isolated by filtration
5. washwashed with ethanol (1 L)
6. customdried under vacuum at 55° C.