1.1: thionyl chloride / dichloromethane / 3 h / 80 °C 2.1: hydrogenchloride; sodium nitrite; NH4BF4 / water / 0.58 h 2.2: 2 h / 20 °C 3.1: sodium hydroxide; water / methanol / 14 h / 60 °C 3.2: pH 6 View Scheme
1: With sodium hydroxide in 1,4-dioxane; water
T=20°C; 16 h; Inert atmosphere;
2: With citric acid in water
pH=~ 4;
参考文献
PFIZER LIMITED; BELL, Andrew Simon; DE GROOT, Marcel John; LEWTHWAITE, Russell Andrew; MARSH, Ian Roger; SCIAMMETTA, Nunzio; STORER, Robert Ian; SWAIN, Nigel Alan
Patent: WO2012/95781 A1, 2012 ;
Location in patent: Page/Page column 100-101 ;
WO 2012/095781 A1