(2,2-二氟苯并[d][1,3]二氧代l-5-基)甲醇合成路线 （共 14 条）
反应条件
1: thionyl chloride / 4-(N,N-dimethlyamino)pyridine / tert-butyl methyl ether / 1.5 h / 15 - 30 °C
2: dimethyl sulfoxide / 1 h / 30 - 40 °C
3: tetra-n-octylammonium bromide; potassium hydroxide / water / 1 h / 70 °C
4: sodium hydroxide; water / ethanol / 80 °C
5: thionyl chloride / toluene / 60 °C
6: triethylamine / dichloromethane / 0 - 20 °C
7: hydrogen / 5 palladium on charcoal / tetrahydrofuran / 96 h / 50 °C / 2250.23 - 3000.3 Torr / autoclave; Inert atmosphere
View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; LOOKER, ADAM; Littler, Benjamin Joseph; Choudhury, Anusuya; Harrison, Cristian; Veluri, Ravikanth; Ryan, Michael P.; Jiang, Licong; Luss-Lusis, Eduard
Patent: US2013/116238 A1, 2013 ;
反应条件
1: thionyl chloride / 4-(N,N-dimethlyamino)pyridine / tert-butyl methyl ether / 1.5 h / 15 - 30 °C
2: dimethyl sulfoxide / 1 h / 30 - 40 °C
3: tetra-n-octylammonium bromide; potassium hydroxide / water / 1 h / 70 °C
View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; LOOKER, ADAM; Littler, Benjamin Joseph; Choudhury, Anusuya; Harrison, Cristian; Veluri, Ravikanth; Ryan, Michael P.; Jiang, Licong; Luss-Lusis, Eduard
Patent: US2013/116238 A1, 2013 ;
反应条件
thionyl chloride; 4-(N,N-dimethlyamino)pyridine in tert-butyl methyl ether
T=15 - 30°C;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2009/73757 A1, 2009 ;
Location in patent: Page/Page column 20 ;
反应条件
thionyl chloride; aq. NaOH; 4-(N,N-dimethlyamino)pyridine in water
参考文献
Vertex Pharmaceuticals Incorported
Patent: US2011/98311 A1, 2011 ;
