2-氨基-5-硝基苯磺酰胺合成路线 （共 14 条）
反应条件
1: trichlorophosphate / acetonitrile; isobutyramide / 3 h / Reflux
2: ammonia / water / 1 h / 20 °C
3: ammonia; (NH4)2CO3; copper(II) sulfate / water / Reflux
View Scheme
参考文献
InterMune, Inc.
Patent: US2011/152246 A1, 2011 ;
反应条件
1.1: N,N-dimethyl-formamide; thionyl chloride / 4 h / Reflux
2.1: ammonium hydroxide / toluene; water; tetrahydrofuran / 2 h / -10 °C / Reflux
2.2: pH 4
3.1: ammonium hydroxide; (NH4)2CO3; copper(II) sulfate / water / 72 h / 118 °C / Autoclave; Industry scale
View Scheme
参考文献
ANADYS PHARMACEUTICALS, INC.
Patent: WO2008/124450 A1, 2008 ;
反应条件
1: 0.5 h / 180 °C
2: sulfuric acid; nitric acid / 21 h / 0 - 20 °C
3: sulfuric acid / 130 °C
View Scheme
参考文献
Ismail, Mohamed A.H.; Abou El Ella, Dalal A.; Abouzid, Khaled A.M.; Mahmoud, Amr H.
Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 7 p. 2455 - 2478
反应条件
1.1: hydrogen / palladium 10 on activated carbon / tetrahydrofuran; methanol / 23 °C / 2585.81 Torr / Industry scale; Autoclave
2.1: pyridine / dichloromethane / 0 - 23 °C / Industry scale
3.1: diethyl ether; isobutyramide / 1 h / 25 °C
4.1: sodium hydroxide; water / 1.5 h / 100 °C
4.2: 0 °C / pH 1 - 2
View Scheme
参考文献
ANADYS PHARMACEUTICALS, INC.
Patent: WO2008/124450 A1, 2008 ;
