外向-8-苄基-8-氮杂双环[3.2.1]辛-3-胺合成路线 （共 32 条）
反应条件
1: 1.) NEt3, ethylchloroformate / 1.) DMF, 2 deg C, 0.5 h; 2.) DMF, 12 h, RT
2: 93 percent / maleic acid, H2 / 10percent Pd/C / aq. ethanol / 7 h / Ambient temperature
3: 77 percent / K2CO3 / acetone / 36 h / Heating
View Scheme
参考文献
Dostert; Imbert; Langlois; et al.
European Journal of Medicinal Chemistry, 1984 , vol. 19, # 2 p. 105 - 110
反应条件
1: sodium carbonate / water; dichloromethane / 0 - 20 °C / |Inert atmosphere
2: phosphorus pentachloride / dichloromethane / 2 h / 0 - 20 °C / |Inert atmosphere
3: dichloromethane; 1,1-dimethylpropan-1-ol / 0 - 20 °C / |Inert atmosphere
4: acetic acid / ethyl acetate / 0.5 h / 80 °C / |Inert atmosphere
5: palladium 10 on activated carbon; hydrogen / methanol / 20 °C / 2585.81 Torr / |Inert atmosphere
View Scheme
参考文献
Asano, Shigehiro; Gavrilyuk, Julia; Burton, Dennis R.; Barbas, Carlos F.
ACS Medicinal Chemistry Letters, 2014 , vol. 5, # 2 p. 133 - 137
