反应条件
1: 1.) diisopropylamine, HMPA, 2.) K2CO3 / 1.) THF, from 0 deg C to 5 deg C, 30 min, 2.) DMF, from 25 deg C to 27 deg C, 16 h
2: 100 percent / HCl / H2O; acetic acid / 1.5 h / 55 - 60 °C
3: 2.) Et3N / 1.) toluene, reflux, 1 h, 2.) toluene, reflux, 21 h
4: 45 percent / NaOH / H2O; methanol / 16 h / 25 - 27 °C
View Scheme
参考文献
Bicking; Bock; Cragoe Jr.; DiPardo; Gould; Holtz; Lee; Robb; Smith; Springer; Blaine
Journal of Medicinal Chemistry, 1983 , vol. 26, # 3 p. 342 - 348