2,5-二溴-4-甲基吡啶合成路线 （共 7 条）
反应条件
1: With hydrogen bromide; bromine; sodium nitrite in water T=0 - 5°C; 1 h; 2: With sodium hydroxide in water pH=~ 13;
参考文献
NEUROCRINE BIOSCIENCES, INC.
Patent: WO2008/124610 A1, 2008 ;
Location in patent: Page/Page column 46 ;
WO 2008/124610 A1
反应条件
acetyl chloride; sodium iodide in acetonitrile T=20°C; 3 h; Inert atmosphere;
参考文献
WO2011/67272 A1, ;
Page/Page column 76 ;
反应条件
1: potassium carbonate / tetrakis(triphenylphosphine) palladium(0) / ethylene glycol dimethyl ether; water / 4 h / 100 °C 2: potassium permanganate / water; acetone / 72 h / 20 °C 3: sulfuric acid / 14 h / Reflux View Scheme
参考文献
Hoffmann-La Roche Inc.; Alam, Muzaffar; Du Bois, Daisy Jo; Hawley, Ronald Charles; Minatti, Ana Elena; Kennedy-Smith, Joshua; Thakkar, Kshitij Chhabilbhai; Wilhelm, Robert Stephen
Patent: US2013/158066 A1, 2013 ;
反应条件
in N,N-dimethyl-formamide T=158°C; 3 h; sealed vessel;
参考文献
SIGNAL PHARMACEUTICALS, LLC; ELSNER, Jan; HARRIS, Roy, L.; LEE, Branden; MORTENSEN, Deborah; PACKARD, Garrick; PAPA, Patrick; PERRIN-NINKOVIC, Sophie; RIGGS, Jennifer; SANKAR, Sabita; SAPIENZA, John; SHEVLIN, Graziella; TEHRANI, Lida; XU, Weiming; ZHAO, Jingjing; PARNES, Jason; MADAKAMUTIL Loui; FULTZ Kimberly; NARLA, Rama K.
Patent: WO2010/62571 A1, 2010 ;
Location in patent: Page/Page column 96 ;
WO 2010/062571 A1
反应条件
copper (I) cyanide in N,N-dimethyl-formamide 20 h; Reflux;
参考文献
Hoffmann-La Roche Inc; Bhagirath, Niala; Brameld, Kenneth Albert; Kennedy-Smith, Joshua
Patent: US2013/90334 A1, 2013 ;
Location in patent: Paragraph 0153 ;
反应条件
1: potassium carbonate / tetrakis(triphenylphosphine) palladium(0) / ethylene glycol dimethyl ether; water / 4 h / 100 °C 2: potassium permanganate / water; acetone / 72 h / 20 °C View Scheme
参考文献
Hoffmann-La Roche Inc.; Alam, Muzaffar; Du Bois, Daisy Jo; Hawley, Ronald Charles; Minatti, Ana Elena; Kennedy-Smith, Joshua; Thakkar, Kshitij Chhabilbhai; Wilhelm, Robert Stephen
Patent: US2013/158066 A1, 2013 ;
反应条件
1.1: acetyl chloride; sodium iodide / acetonitrile / 3 h / 20 °C / Inert atmosphere
2.1: iso-propylmagnesium bromide / tetrahydrofuran / 1 h / -15 - -10 °C
2.2: 1 h / -15 - 0 °C
View Scheme
参考文献
SYNGENTA PARTICIPATIONS AG; CASSAYRE, Jerome Yves; RENOLD, Peter; EL QACEMI, Myriem; PITTERNA, Thomas; TOUEG, Julie Clementine
Patent: WO2011/67272 A1, 2011 ;
Title/Abstract Full Text Show Details
SYNGENTA CROP PROTECTION LLC
Patent: US2012/238517 A1, 2012 ;
