反应条件
1.1: hydroxylamine hydrochloride; pyridine / 0 - 20 °C
2.1: phosphorous pentoxide / water / 1 h / 130 - 140 °C
3.1: phosphorus pentachloride / dichloromethane; toluene / 2 h / Reflux
3.2: 16 h / pH 8 / Cooling with ice
4.1: hydrogen; sodium acetate / palladium 10 on activated carbon / acetic acid / 18 h / 20 °C
5.1: sodium hydroxide / 1,4-dioxane / 18 h / Reflux
5.2: 4 h / 20 °C
6.1: trifluoroacetic acid / dichloromethane / 0.5 h / 20 °C
7.1: thionyl chloride / 0 - 20 °C
View Scheme
参考文献
ELAN PHARMACEUTICALS, INC.; GALEMMO, Robert, A., Jr.; ARTIS, Dean, Richard; YE, Xiaocong, Michael; AUBELE, Danielle, L.; TRUONG, Anh, P.; BOWERS, Simeon; HOM, Roy, K.; ZHU, Yong-Liang; NEITZ, R., Jeffrey; SEALY, Jennifer; ADLER, Marc; BEROZA, Paul; ANDERSON, John, P.
Patent: WO2011/79114 A1, 2011 ;
WO 2011/079114 A1
