4-羟基甲基-7-氮杂吲哚合成路线 (共 11 条)
反应条件
sodium tetrahydroborate; calcium chloride in tetrahydrofuran 6 h; Reflux;
参考文献
ASCEPION PHARMACEUTICALS, INC.; JIANG, Shan; XING, Xinglong; WANG, Qishan; KONG, Ren
Patent: WO2011/23081 A1, 2011 ;
Location in patent: Page/Page column 53 ;
WO 2011/023081 A1
反应条件
1.1: n-heptane; ethylene glycol dimethyl ether / 3 h / 20 °C 2.1: trichlorophosphate / 85 - 90 °C 2.2: pH 9 3.1: zinc / tris-(dibenzylideneacetone)dipalladium(0); [Fe(II)(C5H5)(C5H4PPh2)] / isobutyramide / 2 h / 120 °C / Inert atmosphere 4.1: sodium hydroxide; water / ethanol / 6 h / Reflux 5.1: trichlorophosphate / Reflux 5.2: pH 9 6.1: calcium chloride; sodium tetrahydroborate / tetrahydrofuran / 6 h / Reflux View Scheme
参考文献
WO2011/23081 A1, ;
WO 2011/023081 A1
反应条件
1.1: zinc / tris-(dibenzylideneacetone)dipalladium(0); [Fe(II)(C5H5)(C5H4PPh2)] / isobutyramide / 2 h / 120 °C / Inert atmosphere 2.1: sodium hydroxide; water / ethanol / 6 h / Reflux 3.1: trichlorophosphate / Reflux 3.2: pH 9 4.1: calcium chloride; sodium tetrahydroborate / tetrahydrofuran / 6 h / Reflux View Scheme
参考文献
WO2011/23081 A1, ;
WO 2011/023081 A1
反应条件
1.1: sodium hydroxide; water / ethanol / 6 h / Reflux 2.1: trichlorophosphate / Reflux 2.2: pH 9 3.1: calcium chloride; sodium tetrahydroborate / tetrahydrofuran / 6 h / Reflux View Scheme
参考文献
WO2011/23081 A1, ;
WO 2011/023081 A1
反应条件
1.1: trichlorophosphate / Reflux 1.2: pH 9 2.1: calcium chloride; sodium tetrahydroborate / tetrahydrofuran / 6 h / Reflux View Scheme
参考文献
WO2011/23081 A1, ;
WO 2011/023081 A1
反应条件
1: With thionyl chloride in dichloromethane T=20°C; 2: With potassium carbonate in water pH=9;
参考文献
ASCEPION PHARMACEUTICALS, INC.; JIANG, Shan; XING, Xinglong; WANG, Qishan; KONG, Ren
Patent: WO2011/23081 A1, 2011 ;
Location in patent: Page/Page column 53 ;
WO 2011/023081 A1
反应条件
sodium tetrahydroborate; calcium chloride in tetrahydrofuran
6 h; Reflux;
参考文献
ASCEPION PHARMACEUTICALS, INC.; JIANG, Shan; XING, Xinglong; WANG, Qishan; KONG, Ren
Patent: WO2011/23081 A1, 2011 ;
Location in patent: Page/Page column 53 ;
WO 2011/023081 A1
反应条件
1.1: n-heptane; ethylene glycol dimethyl ether / 3 h / 20 °C
2.1: trichlorophosphate / 85 - 90 °C
2.2: pH 9
3.1: zinc / tris-(dibenzylideneacetone)dipalladium(0); [Fe(II)(C5H5)(C5H4PPh2)] / isobutyramide / 2 h / 120 °C / Inert atmosphere
4.1: sodium hydroxide; water / ethanol / 6 h / Reflux
5.1: trichlorophosphate / Reflux
5.2: pH 9
6.1: calcium chloride; sodium tetrahydroborate / tetrahydrofuran / 6 h / Reflux
View Scheme
参考文献
ASCEPION PHARMACEUTICALS, INC.; JIANG, Shan; XING, Xinglong; WANG, Qishan; KONG, Ren
Patent: WO2011/23081 A1, 2011 ;
WO 2011/023081 A1
反应条件
1.1: zinc / tris-(dibenzylideneacetone)dipalladium(0); [Fe(II)(C5H5)(C5H4PPh2)] / isobutyramide / 2 h / 120 °C / Inert atmosphere
2.1: sodium hydroxide; water / ethanol / 6 h / Reflux
3.1: trichlorophosphate / Reflux
3.2: pH 9
4.1: calcium chloride; sodium tetrahydroborate / tetrahydrofuran / 6 h / Reflux
View Scheme
参考文献
ASCEPION PHARMACEUTICALS, INC.; JIANG, Shan; XING, Xinglong; WANG, Qishan; KONG, Ren
Patent: WO2011/23081 A1, 2011 ;
WO 2011/023081 A1
反应条件
1.1: sodium hydroxide; water / ethanol / 6 h / Reflux
2.1: trichlorophosphate / Reflux
2.2: pH 9
3.1: calcium chloride; sodium tetrahydroborate / tetrahydrofuran / 6 h / Reflux
View Scheme
参考文献
ASCEPION PHARMACEUTICALS, INC.; JIANG, Shan; XING, Xinglong; WANG, Qishan; KONG, Ren
Patent: WO2011/23081 A1, 2011 ;
WO 2011/023081 A1