5-溴-1,3-二氟-2-硝基苯合成路线 （共 5 条）
反应条件
sodium perborate; acetic acid T=65 - 70°C; 21 h; Inert atmosphere;
参考文献
Rueeger, Heinrich; Lueoend, Rainer; Rogel, Olivier; Rondeau, Jean-Michel; Moebitz, Henrik; MacHauer, Rainer; Jacobson, Laura; Staufenbiel, Matthias; Desrayaud, Sandrine; Neumann, Ulf
Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3364 - 3386
反应条件
hydrogen bromide; copper(I) bromide; sodium nitrite 1.) 0 deg C, 2.) 3 h; Multistep reaction;
参考文献
Journal of Organic Chemistry USSR (English Translation), , vol. 28, # 7 p. 1140 - 1147
Zhurnal Organicheskoi Khimii, , vol. 28, # 7 p. 1445 - 1454
反应条件
1-methyl-pyrrolidin-2-one
T=160 - 165°C; 6 h; Inert atmosphere;
参考文献
Rueeger, Heinrich; Lueoend, Rainer; Rogel, Olivier; Rondeau, Jean-Michel; Moebitz, Henrik; MacHauer, Rainer; Jacobson, Laura; Staufenbiel, Matthias; Desrayaud, Sandrine; Neumann, Ulf
Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3364 - 3386
反应条件
potassium hydroxide
T=90°C; 1 h;
参考文献
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Patent: WO2009/42711 A1, 2009 ;
Location in patent: Page/Page column 364-365 ;
WO 2009/042711 A1
反应条件
1.1: 1-methyl-pyrrolidin-2-one / 6 h / 160 - 165 °C / Inert atmosphere
2.1: thionyl chloride / 0 - 25 °C / Inert atmosphere
3.1: diisobutylaluminium hydride / tetrahydrofuran; hexane / 4 h / 0 - 5 °C / Inert atmosphere
3.2: 0.5 h / 25 °C / Cooling with ice; Inert atmosphere
View Scheme
参考文献
Rueeger, Heinrich; Lueoend, Rainer; Rogel, Olivier; Rondeau, Jean-Michel; Moebitz, Henrik; MacHauer, Rainer; Jacobson, Laura; Staufenbiel, Matthias; Desrayaud, Sandrine; Neumann, Ulf
Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3364 - 3386
