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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
380380-59-6
合成路线
(共 7 条)
380380-60-9
5-溴-2-(1H-四唑-5-基)吡啶
→
反应条件
380380-59-6
反应条件
1: With acetic anhydride in pyridine T=20 - 130°C; 1.5 h; 2: With hydrogenchloride in pyridine; water pH=3 - 4;
参考文献
Gordeev, Mikhail Fedorovich; Yuan, Zhengyu; Liu, Jinqian; Wang, Qiang
Patent: US2010/69441 A1, 2010 ;
Location in patent: Page/Page column 39 ;
944718-28-9
→
反应条件
380380-59-6
反应条件
triethylamine; p-toluenesulfonyl chloride in dichloromethane; acetonitrile T=25°C; 5 h;
参考文献
SCHERING CORPORATION
Patent: WO2007/84451 A1, 2007 ;
Location in patent: Page/Page column 164 ;
WO 2007/084451 A1
108-24-7
乙酸酐
+
380380-60-9
5-溴-2-(1H-四唑-5-基)吡啶
→
反应条件
380380-59-6
反应条件
pyridine 3 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
18871-66-4
1,1-二甲氧基-N,N-二甲基乙胺
+
848952-82-9
5-溴-2-吡啶甲酰肼
→
反应条件
380380-59-6
反应条件
1: in N,N-dimethyl-formamide T=60°C; 2.5 h; 2: With toluene-4-sulfonic acid in toluene 3 h; Heating / reflux;
参考文献
PFIZER LIMITED
Patent: WO2006/100588 A1, 2006 ;
Location in patent: Page/Page column 44 ;
WO 2006/100588 A1
848952-82-9
5-溴-2-吡啶甲酰肼
+
64-19-7
醋酸
→
反应条件
380380-59-6
反应条件
1: With trichlorophosphate T=100 - 120°C; 2.5 h; 2: With sodium hydrogencarbonate in ethyl acetate
参考文献
LOCUS PHARMACEUTICALS, INC.
Patent: US2010/41642 A1, 2010 ;
Location in patent: Page/Page column 25 ;
624-28-2
2,5-二溴吡啶
→
反应条件
380380-59-6
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: pyridine / 3 h / 150 °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
97483-77-7
5-溴-2-氰基吡啶
→
反应条件
380380-59-6
反应条件
1: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 3 h / 110 °C / Inert atmosphere 2: pyridine / 3 h / 150 °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