反应条件
1: 1.) 2.2 M n-butyllithium, 2.) hexachloroethane / 1.) Et2O, reflux, 2.5 h, 2.) Et2O, THF, form -65 deg C to RT
2: 67 percent / AlCl3 / 1,2-dichloro-ethane / 1.) from 5 deg C to RT, 30 min, 2.) reflux, 30 min
3: 76 percent / hydroxylamine hydrochloride, pyridine / 24 h / Heating
4: 98 percent / 1 h / Heating
5: 84 percent / sodium hydride / dimethylformamide / 0.67 h / 30 °C
6: 91 percent / pyridine hydrochloride / 2 h / 180 °C
7: K2CO3 / dimethylformamide / 1.) 60 deg C, 2 h, 2.) from 60 deg C to RT, overnight
8: 63 percent / 5percent aq. NaOH / ethanol / 0.5 h / Heating
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
