5-碘-1-甲基-1H-吲哚合成路线 （共 5 条）
反应条件
1: 5-iodo-1H-indole With sodium hydride in tetrahydrofuran T=-78°C; 1 h; 2: methyl iodide in tetrahydrofuran T=25°C; 16 h; Further stages.;
参考文献
Abbott Laboratories
Patent: US2004/116518 A1, 2004 ;
Location in patent: Page 79 ;
反应条件
triethyl borane; oxygen; N-ethylpiperidinium hypophosphite in 1,4-dioxane; hexane T=73°C; 2 h; Air atmosphere;
参考文献
Gray, Vincent James; Wilden, Jonathan D.
Tetrahedron Letters, 2012 , vol. 53, # 1 p. 41 - 44
反应条件
(tBuCN)2CuOTf; silver fluoride in N,N-dimethyl-formamide T=140°C; 22 h; Inert atmosphere;
参考文献
Fier, Patrick S.; Hartwig, John F.
Journal of the American Chemical Society, 2012 , vol. 134, # 26 p. 10795 - 10798
反应条件
1: With bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide in dichloromethane
Sonogashira Coupling; 3 h;
2: With sodium hydroxide in tetrahydrofuran; methanol
T=20°C;
参考文献
BIONOMICS LIMITED
Patent: WO2008/70908 A1, 2008 ;
Location in patent: Page/Page column 55; 56 ;
反应条件
1: copper(l) iodide; bis-triphenylphosphine-palladium(II) chloride / 1,4-dioxane / 1 h / Inert atmosphere
2: tetrabutyl ammonium fluoride / tetrahydrofuran / 0.25 h
View Scheme
参考文献
Flynn, Bernard L.; Gill, Gurmit S.; Grobelny, Damian W.; Chaplin, Jason H.; Paul, Dharam; Leske, Annabell F.; Lavranos, Tina C.; Chalmers, David K.; Charman, Susan A.; Kostewicz, Edmund; Shackleford, David M.; Morizzi, Julia; Hamel, Ernest; Jung, M. Katherine; Kremmidiotis, Gabriel
Journal of Medicinal Chemistry, 2011 , vol. 54, # 17 p. 6014 - 6027
