2-甲基-5-(5-溴吡啶-2-基)四氮唑合成路线 （共 10 条）
反应条件
sodium hydroxide in DMF (N,N-dimethyl-formamide) T=0 - 20°C; 2 h;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2004/56818 A1, 2004 ;
Location in patent: Page 52-53 ;
WO 2004/056818 A1
反应条件
sodium hydroxide; methyl iodide in tetrahydrofuran; N,N-dimethyl-formamide T=48°C; Cooling with ice/brine;
参考文献
TRIUS THERAPEUTICS; COSTELLO, Carrie, A.; SIMSON, Jaqueline, A.; DUGUID, Robert, J.; PHILLIPSON, Douglas
Patent: WO2010/42887 A2, 2010 ;
Location in patent: Page/Page column 15-16 ;
反应条件
sodium hydroxide in N,N-dimethyl-formamide T=0 - 20°C; Inert atmosphere;
参考文献
Im, Weon Bin; Choi, Sun Ho; Park, Ju-Young; Choi, Sung Hak; Finn, John; Yoon, Sung-Hwa
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1027 - 1039
反应条件
1: sodium azide / dimethylformamide / 4 h / 120 °C 2: 2.2 g / KOH / dimethylformamide / 24 h / 20 °C View Scheme
参考文献
ASTRAZENECA UK LIMITED
Patent: WO2005/116023 A1, 2005 ;
Location in patent: Page/Page column 67 ;
WO 2005/116023 A1
反应条件
N-ethyl-N,N-diisopropylamine in methanol; acetonitrile T=0°C; 1.5 h;
参考文献
Clark, Richard F.; Djuric, Stevan; Ma, Zhenkun; Phan, Ly; Rupp, Michael
Patent: US2004/33970 A1, 2004 ;
Location in patent: Page/Page column 9 ;
反应条件
1: 65 percent / NaCN / dimethylformamide / 3 h / Heating 2: sodium azide / dimethylformamide / 4 h / 120 °C 3: 2.2 g / KOH / dimethylformamide / 24 h / 20 °C View Scheme
参考文献
Jo, Yeong Woo; Im, Weon Bin; Rhee, Jae Keol; Shim, Mi Ja; Kim, Won Bae; Choi, Eung Chil
Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 22 p. 5909 - 5915
反应条件
1: sodium cyanide / N,N-dimethyl-formamide / 7 h / 150 °C / Inert atmosphere 2: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 3 h / 110 °C / Inert atmosphere 3: sodium hydroxide / N,N-dimethyl-formamide / 0 - 20 °C / Inert atmosphere View Scheme
参考文献
Im, Weon Bin; Choi, Sun Ho; Park, Ju-Young; Choi, Sung Hak; Finn, John; Yoon, Sung-Hwa
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1027 - 1039
反应条件
1: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 3 h / 110 °C / Inert atmosphere 2: sodium hydroxide / N,N-dimethyl-formamide / 0 - 20 °C / Inert atmosphere View Scheme
参考文献
Im, Weon Bin; Choi, Sun Ho; Park, Ju-Young; Choi, Sung Hak; Finn, John; Yoon, Sung-Hwa
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1027 - 1039
反应条件
lithium chloride; bis-triphenylphosphine-palladium(II) chloride in 1-methyl-pyrrolidin-2-one T=20 - 120°C; 4 h;
参考文献
Im, Weon Bin; Choi, Sun Ho; Park, Ju-Young; Choi, Sung Hak; Finn, John; Yoon, Sung-Hwa
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1027 - 1039
反应条件
potassium carbonate; tris-(dibenzylideneacetone)dipalladium(0); tri-cyclo-hexyl-phosphine in 1,4-dioxane; water T=70°C; 1 h; Inert atmosphere;
参考文献
TRIUS THERAPEUTICS; COSTELLO, Carrie, A.; SIMSON, Jaqueline, A.; DUGUID, Robert, J.; PHILLIPSON, Douglas
Patent: WO2010/42887 A2, 2010 ;
Location in patent: Page/Page column 18-19 ;
