4-[[5-氨基-1-(2,6-二氟苯甲酰基)-1H-1,2,4-三唑-3-基]氨基]苯磺酰胺合成路线 （共 7 条）
反应条件
1: cyanocarbonimidic acid diphenyl ester; 4-aminobenzene sulfonamide With pyridine T=20 - 30°C; 10 h; 2: 2,6-difluorobenzoic hydrazide T=70 - 80°C; 4 h; 3: With ammonium chloride in water T=55 - 60°C;
参考文献
JANSSEN PHARMACEUTICA, N.V.
Patent: WO2005/77922 A2, 2005 ;
Location in patent: Page/Page column 46-47 ;
WO 2005/077922 A2
反应条件
1: in DMF (N,N-dimethyl-formamide) T=20 - 110°C; 3.5 h; 2: With water in DMF (N,N-dimethyl-formamide) Product distribution / selectivity;
参考文献
JANSSEN PHARMACEUTICA, N.V.
Patent: WO2005/77922 A2, 2005 ;
Location in patent: Page/Page column 54-55 ;
WO 2005/077922 A2
反应条件
pyridine T=20°C; 6 h;
参考文献
Lin, Ronghui; Connolly, Peter J.; Huang, Shenlin; Wetter, Steven K.; Lu, Yanhua; Murray, William V.; Emanuel, Stuart L.; Gruninger, Robert H.; Fuentes-Pesquera, Angel R.; Rugg, Catherine A.; Middleton, Steven A.; Jolliffe, Linda K.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 13 p. 4208 - 4211
反应条件
1: hydrazine / tetrahydrofuran / 2 h / 70 °C 2: 50.2 mg / pyridine / 6 h / 20 °C View Scheme
参考文献
Lin, Ronghui; Connolly, Peter J.; Huang, Shenlin; Wetter, Steven K.; Lu, Yanhua; Murray, William V.; Emanuel, Stuart L.; Gruninger, Robert H.; Fuentes-Pesquera, Angel R.; Rugg, Catherine A.; Middleton, Steven A.; Jolliffe, Linda K.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 13 p. 4208 - 4211
反应条件
1: hydrazine / tetrahydrofuran / 3 h / 50 - 60 °C 2: 50.2 mg / pyridine / 6 h / 20 °C View Scheme
参考文献
Lin, Ronghui; Connolly, Peter J.; Huang, Shenlin; Wetter, Steven K.; Lu, Yanhua; Murray, William V.; Emanuel, Stuart L.; Gruninger, Robert H.; Fuentes-Pesquera, Angel R.; Rugg, Catherine A.; Middleton, Steven A.; Jolliffe, Linda K.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 13 p. 4208 - 4211
反应条件
1: KOH / dimethylformamide / 1 h / 50 - 60 °C 2: hydrazine / tetrahydrofuran / 3 h / 50 - 60 °C 3: 50.2 mg / pyridine / 6 h / 20 °C View Scheme
参考文献
Lin, Ronghui; Connolly, Peter J.; Huang, Shenlin; Wetter, Steven K.; Lu, Yanhua; Murray, William V.; Emanuel, Stuart L.; Gruninger, Robert H.; Fuentes-Pesquera, Angel R.; Rugg, Catherine A.; Middleton, Steven A.; Jolliffe, Linda K.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 13 p. 4208 - 4211
反应条件
1: tetrahydrofuran / Heating 2: hydrazine / tetrahydrofuran / 2 h / 70 °C 3: 50.2 mg / pyridine / 6 h / 20 °C View Scheme
参考文献
Lin, Ronghui; Connolly, Peter J.; Huang, Shenlin; Wetter, Steven K.; Lu, Yanhua; Murray, William V.; Emanuel, Stuart L.; Gruninger, Robert H.; Fuentes-Pesquera, Angel R.; Rugg, Catherine A.; Middleton, Steven A.; Jolliffe, Linda K.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 13 p. 4208 - 4211
