7-氮杂吲哚-7-氧化物合成路线 （共 49 条）
反应条件
1.1: [14C]-Tetramethylammonium bromide; trifluoromethanesulfonic anhydride / N,N-dimethyl-formamide / 24.5 h / 0 - 20 °C / Inert atmosphere 1.2: pH 7 2.1: sodium hydroxide / tetra(n-butyl)ammonium hydrogensulfate / dichloromethane / 1 h / 20 °C View Scheme
参考文献
ASTRAZENECA AB
Patent: US2011/306613 A1, 2011 ;
反应条件
methanesulfonyl chloride in N,N-dimethyl-formamide T=50 - 73°C; 2 h;
参考文献
INCYTE CORPORATION
Patent: WO2006/69080 A2, 2006 ;
Location in patent: Page/Page column 35 ;
WO 2006/069080 A2
反应条件
in N,N-dimethyl-formamide T=50 - 72°C;
参考文献
ASTEX THERAPEUTICS LIMITED; THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL; CANCER RESEARCH TECHNOLOGY LIMITED; ASTRAZENECA AB
Patent: WO2007/125325 A1, 2007 ;
Location in patent: Page/Page column 86 ;
WO 2007/125325 A1
反应条件
trichlorophosphate in water
参考文献
Amgen Inc.
Patent: US6878714 B2, 2005 ;
US 6878714 B2
反应条件
in trichlorophosphate
参考文献
Liang, Congxin; Sun, Li; Wei, Chung Chen; Tang, Peng Cho; McMahon, Gerald; Hirth, Klaus Peter; Cui, Jingrong
Patent: US2002/183319 A1, 2002 ;
US 20020183319 A1
反应条件
in trichlorophosphate
参考文献
Liang, Congxin; Sun, Li; Wei, Chung Chen; Tang, Peng Cho; McMahon, Gerald; Hirth, Klaus Peter; Cui, Jingrong
Patent: US2002/183319 A1, 2002 ;
US 20020183319 A1
反应条件
1: 1H-pyrrolo[2,3-b]pyridine 7-oxide With trimethylsilyl iodide; lithium hexamethyldisilazane in tetrahydrofuran Inert atmosphere; 2: methyl chloroformate in tetrahydrofuran T=20°C; 5 h;
参考文献
Almirall, S.A.; Vidal Juan, Bernat; Alonso Diez, Juan Antonio; Buil Albero, María Antonia; Eastwood, Paul Robert; Esteve Trias, Cristina; Lozoya Toribio, María Estrella; Roberts, Richard Spurring; Vidal Gispert, Laura
Patent: EP2548876 A1, 2013 ;
Location in patent: Paragraph 0531 ;
EP 2548876 A1
反应条件
1.1: [14C]-Tetramethylammonium bromide; trifluoromethanesulfonic anhydride / N,N-dimethyl-formamide / 24.5 h / 0 - 20 °C / Inert atmosphere 1.2: pH 7 2.1: sodium hydroxide / tetra(n-butyl)ammonium hydrogensulfate / dichloromethane / 1 h / 20 °C 3.1: potassium acetate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / N,N-dimethyl-formamide / 24 h / 90 °C / Inert atmosphere View Scheme
参考文献
ASTRAZENECA AB
Patent: US2011/306613 A1, 2011 ;
反应条件
1.1: methanesulfonyl chloride / N,N-dimethyl-formamide / 2 h / 70 °C 2.1: sodium hydride / tetrahydrofuran; mineral oil / 0.5 h / 0 °C / |Inert atmosphere 2.2: 50 °C / |Inert atmosphere 3.1: sec.-butyllithium / tetrahydrofuran; cyclohexane / 0.5 h / 78 °C / |Inert atmosphere 3.2: 2 h 4.1: potassium fluoride / methanol / 1 h / 20 °C View Scheme
参考文献
Gehringer, Matthias; Pfaffenrot, Ellen; Bauer, Silke; Laufer, Stefan A.
ChemMedChem, 2014 , vol. 9, # 2 p. 277 - 281
反应条件
triethylamine in acetonitrile 144 h; Reflux;
参考文献
Pillard, Christelle; Bassene, Carine Ekambome; Suzenet, Franck; Guillaumet, Gerald
Synthesis, 2008 , # 13 p. 2049 - 2054
