1-[(4-甲基苯基)磺酰基]-3-(4,4,5,5-四甲基-1,3,2-二氧硼烷)-1H-吡咯并[2,3-b]吡啶合成路线 （共 6 条）
反应条件
potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride in ethylene glycol dimethyl ether T=90°C; 18 h; Heating / reflux;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED?
Patent: WO2005/95400 A1, 2005 ;
Location in patent: Page/Page column 326; 327 ;
WO 2005/095400 A1
反应条件
in dichloromethane T=20 - 30°C; Large scale;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; TAYLOR, Lori, Kell; SEWELL, Kathryn, Lea; HOOCK, Thomas, Carl
Patent: WO2014/74471 A1, 2014 ;
Location in patent: Paragraph 0278-0280 ;
反应条件
1: n-butyllithium / tetrahydrofuran / 0.5 h / -90 - -80 °C / |Large scale 2: dichloromethane / 1.08 h / 20 - 30 °C / |Large scale View Scheme
反应条件
1.1: bromine / N,N-dimethyl-formamide / 2.67 h / 0 - 10 °C / |Large scale 2.1: sodium hydride / tetrahydrofuran / 10 - 20 °C / |Large scale 2.2: 1.5 h / 10 - 20 °C / |Large scale 3.1: n-butyllithium / tetrahydrofuran / 0.5 h / -90 - -80 °C / |Large scale 4.1: dichloromethane / 1.08 h / 20 - 30 °C / |Large scale View Scheme
反应条件
1.1: sodium hydride / tetrahydrofuran / 10 - 20 °C / |Large scale 1.2: 1.5 h / 10 - 20 °C / |Large scale 2.1: n-butyllithium / tetrahydrofuran / 0.5 h / -90 - -80 °C / |Large scale 3.1: dichloromethane / 1.08 h / 20 - 30 °C / |Large scale View Scheme
反应条件
potassium carbonate; tetrakis(triphenylphosphine) palladium(0) in ethylene glycol dimethyl ether; water
T=170°C; 0.166667 h; Microwave heating;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2005/103050 A2, 2005 ;
Location in patent: Page/Page column 183-184 ;
WO 2005/103050 A2
