4-溴-1-(4-氟苯基)-1H-吡唑并[3,4-c]吡啶合成路线 （共 3 条）
反应条件
1: 4-bromo-1-(4-fluorophenyl)-1H-pyrazolo[3,4-c]pyridine With isopropylmagnesium chloride in tetrahydrofuran T=-20 - -10°C; 2: carbon dioxide in tetrahydrofuran T=22°C; 3: With hydrogenchloride; water pH=6 - 7;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; COOK, Brian Nicholas; DISALVO, Darren; FANDRICK, Daniel Robert; HARCKEN, Christian; KUZMICH, Daniel; LEE, Thomas Wai-Ho; LIU, Pingrong; LORD, John; MAO, Can; NEU, Jochen; RAUDENBUSH, Brian Christopher; RAZAVI, Hossein; REEVES, Jonathan Timothy; SONG, Jinhua, J.; SWINAMER, Alan, David; TAN, Zhulin
Patent: WO2010/36632 A1, 2010 ;
Location in patent: Page/Page column 155; 156 ;
反应条件
1: in 1-methyl-pyrrolidin-2-one
T=20°C; 2 h;
2: With potassium hydroxide in 1-methyl-pyrrolidin-2-one; water
T=80°C; 0.5 - 1 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; COOK, Brian Nicholas; DISALVO, Darren; FANDRICK, Daniel Robert; HARCKEN, Christian; KUZMICH, Daniel; LEE, Thomas Wai-Ho; LIU, Pingrong; LORD, John; MAO, Can; NEU, Jochen; RAUDENBUSH, Brian Christopher; RAZAVI, Hossein; REEVES, Jonathan Timothy; SONG, Jinhua, J.; SWINAMER, Alan, David; TAN, Zhulin
Patent: WO2010/36632 A1, 2010 ;
Location in patent: Page/Page column 155 ;
反应条件
potassium carbonate; trans-N,N'-dimethylcyclohexane-1,2-diamine; copper(l) iodide in 1-methyl-pyrrolidin-2-one
T=120°C; 0.5 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; COOK, Brian Nicholas; DISALVO, Darren; FANDRICK, Daniel Robert; HARCKEN, Christian; KUZMICH, Daniel; LEE, Thomas Wai-Ho; LIU, Pingrong; LORD, John; MAO, Can; NEU, Jochen; RAUDENBUSH, Brian Christopher; RAZAVI, Hossein; REEVES, Jonathan Timothy; SONG, Jinhua, J.; SWINAMER, Alan, David; TAN, Zhulin
Patent: WO2010/36632 A1, 2010 ;
Location in patent: Page/Page column 109 ;
