7-溴-2,3,4,5-四氢-1H-苯并[d]氮杂卓合成路线 （共 5 条）
反应条件
1: With formic acid T=25 - 70°C; 2: With sodium hydroxide in water
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HOFFMANN, Matthias; BISCHOFF, Daniel; DAHMANN, Georg; KLICIC, Jasna; SCHAENZLE, Gerhard; WOLLIN, Stefan Ludwig Michael; CONVERS-REIGNIER, Serge Gaston; EAST, Stephen Peter; MARLIN, Frederic Jacques; McCARTHY, Clive; SCOTT, John
Patent: US2013/29949 A1, 2013 ;
Location in patent: Paragraph 0197; 0198; 0199 ;
反应条件
1: With sodium azide; methanesulfonic acid
T=0 - 20°C;
2: With dimethylsulfide borane complex in tetrahydrofuran
T=0°C; 7 h; Reflux;
参考文献
MILLENNIUM PHARMACEUTICALS, INC.; BLACKBURN, Christopher; CIAVARRI, Jeffrey; GIGSTAD, Kenneth; XU, He
Patent: WO2010/151318 A1, 2010 ;
Location in patent: Page/Page column 143-144 ;
WO 2010/151318 A1
反应条件
1: With hydrogen bromide; sodium nitrite in water
T=0°C;
2: With hydrogen bromide; copper(I) bromide in water
Sandmeyer reaction;
参考文献
Shah, Unmesh; Lankin, Claire M.; Boyle, Craig D.; Chackalamannil, Samuel; Greenlee, William J.; Neustadt, Bernard R.; Cohen-Williams, Mary E.; Higgins, Guy A.; Ng, Kwokei; Varty, Geoffrey B.; Zhang, Hongtao; Lachowicz, Jean E.
Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 14 p. 4204 - 4209
反应条件
1: With sodium azide; methanesulfonic acid
T=25°C; Schmidt Reaction; 2 h; Cooling with ice;
2: With dimethylsulfide borane complex in 1,2-dichloro-ethane
T=80°C;
参考文献
Blackburn, Christopher; Barrett, Cynthia; Chin, Janice; Garcia, Kris; Gigstad, Kenneth; Gould, Alexandra; Gutierrez, Juan; Harrison, Sean; Hoar, Kara; Lynch, Chrissie; Rowland, R. Scott; Tsu, Chris; Ringeling, John; Xu, He
Journal of Medicinal Chemistry, 2013 , vol. 56, # 18 p. 7201 - 7211
参考文献
Hagen, Susan; Josyula, Vara Prasad Venkata Nagendra
Patent: US2005/70523 A1, 2005 ;
Location in patent: Page/Page column 24 ;
