反应条件
1: 78 percent / AlCl3 / 1,2-dichloro-ethane / 1.) from 5 deg C to RT, 30 min, 2.) reflux, 30 min
2: 95 percent / hydroxylamine hydrochloride, pyridine / 24 h / Heating
3: 85 percent / 1 h / Heating
4: 90 percent / sodium hydride / dimethylformamide / 0.67 h / 30 °C
5: 1.) 2.2 M n-butyllithium, 2.) bromine / 1.) THF, -40 deg C, 2 h
6: pyridine hydrochloride / 2 h / 180 °C
7: K2CO3 / dimethylformamide / 1.) 60 deg C, 2 h, 2.) from 60 deg C to RT, overnight
8: aq. NaOH / dimethylformamide / 1.5 h / 90 °C
View Scheme
参考文献
Shutske, Gregory M.; Setescak, Linda L.; Allen, Richard C.; Davis, Larry; Effland, Richard C.; et al.
Journal of Medicinal Chemistry, 1982 , vol. 25, # 1 p. 36 - 44
