6-氯-2,3,4,9-四氢-1H-咔唑-1-羧酰胺合成路线 （共 5 条）
反应条件
ammonia in ethanol T=60°C; 24 h;
参考文献
ELIXIR PHARMACEUTICALS, INC.
Patent: US2005/256181 A1, 2005 ;
Location in patent: Page/Page column 20 ;
反应条件
sulfuric acid T=20°C; 2 h;
参考文献
Napper, Andrew D.; Hixon, Jeffrey; McDonagh, Thomas; Keavey, Kenneth; Pons, Jean-Francois; Barker, Jonathan; Yau, Wei Tsung; Amouzegh, Patricia; Flegg, Adam; Hamelin, Estelle; Thomas, Russell J.; Kates, Michael; Jones, Stephen; Navia, Manuel A.; Saunders, Jeffrey O.; DiStefano, Peter S.; Curtis, Rory
Journal of Medicinal Chemistry, 2005 , vol. 48, # 25 p. 8045 - 8054
反应条件
1: 100 percent / Br2 / diethyl ether / 1.5 h / 0 - 20 °C 2: 77 percent / 3 h / 150 °C 3: 91 percent / aq. NaOH / ethanol / 1 h / 20 °C 4: 64 percent / EDC; HOBt / CH2Cl2 / 20 °C 5: 71 percent / H2SO4 / 2 h / 20 °C View Scheme
参考文献
SIENA BIOTECH S.P.A.; DIODATO, Enrica; MARCUCCI, Katia; THOMAS, Russell; WIEDENAU, Paul; RETTIG, Martin; ROBERTS, Huw
Patent: WO2013/57258 A1, 2013 ;
反应条件
1: 77 percent / 3 h / 150 °C 2: 91 percent / aq. NaOH / ethanol / 1 h / 20 °C 3: 64 percent / EDC; HOBt / CH2Cl2 / 20 °C 4: 71 percent / H2SO4 / 2 h / 20 °C View Scheme
参考文献
Napper, Andrew D.; Hixon, Jeffrey; McDonagh, Thomas; Keavey, Kenneth; Pons, Jean-Francois; Barker, Jonathan; Yau, Wei Tsung; Amouzegh, Patricia; Flegg, Adam; Hamelin, Estelle; Thomas, Russell J.; Kates, Michael; Jones, Stephen; Navia, Manuel A.; Saunders, Jeffrey O.; DiStefano, Peter S.; Curtis, Rory
Journal of Medicinal Chemistry, 2005 , vol. 48, # 25 p. 8045 - 8054
反应条件
1: 64 percent / EDC; HOBt / CH2Cl2 / 20 °C 2: 71 percent / H2SO4 / 2 h / 20 °C View Scheme
参考文献
Napper, Andrew D.; Hixon, Jeffrey; McDonagh, Thomas; Keavey, Kenneth; Pons, Jean-Francois; Barker, Jonathan; Yau, Wei Tsung; Amouzegh, Patricia; Flegg, Adam; Hamelin, Estelle; Thomas, Russell J.; Kates, Michael; Jones, Stephen; Navia, Manuel A.; Saunders, Jeffrey O.; DiStefano, Peter S.; Curtis, Rory
Journal of Medicinal Chemistry, 2005 , vol. 48, # 25 p. 8045 - 8054
