5-氨基-3-(三氟甲基)氰基吡啶合成路线 (共 6 条)
反应条件
1: in N,N-dimethyl acetamide T=60°C; 2: With hydrogenchloride in methanol; N,N-dimethyl acetamide; water 2 h; Heating / reflux; Product distribution / selectivity;
参考文献
SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
Patent: WO2008/119015 A2, 2008 ;
Location in patent: Page/Page column 54 ;
反应条件
trifluoroacetic acid in dichloromethane
T=20°C; 2 h; Product distribution / selectivity;
参考文献
SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
Patent: WO2008/119015 A2, 2008 ;
Location in patent: Page/Page column 51 ;
反应条件
iron; acetic acid in ethyl acetate
T=65°C; 2 h; Product distribution / selectivity;
参考文献
SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
Patent: WO2008/119015 A2, 2008 ;
Location in patent: Page/Page column 47-48 ;
反应条件
1: trichlorophosphate / N,N-dimethyl-formamide / 4 h / 110 °C
2: sodium t-butanolate / 9,9-dimethyl-4,5-bis(diphenyl-phosphino)xanthene; tris-(dibenzylideneacetone)dipalladium(0) / toluene / 2 h / Inert atmosphere; Reflux
3: 1,1'-bis-(diphenylphosphino)ferrocene; tris-(dibenzylideneacetone)dipalladium(0) / N,N-dimethyl-formamide / 0.5 h / 170 °C / Reflux; Inert atmosphere
4: trifluoroacetic acid / dichloromethane / 3 h / 20 °C
View Scheme
参考文献
ARAGON PHARMACEUTICALS, INC.; SMITH, Nicholas, D.; BONNEFOUS, Celine; JULIEN, Jackaline, D.
Patent: WO2011/103202 A2, 2011 ;
WO 2011/103202 A2
反应条件
1: sodium t-butanolate / 9,9-dimethyl-4,5-bis(diphenyl-phosphino)xanthene; tris-(dibenzylideneacetone)dipalladium(0) / toluene / 2 h / Inert atmosphere; Reflux
2: 1,1'-bis-(diphenylphosphino)ferrocene; tris-(dibenzylideneacetone)dipalladium(0) / N,N-dimethyl-formamide / 0.5 h / 170 °C / Reflux; Inert atmosphere
3: trifluoroacetic acid / dichloromethane / 3 h / 20 °C
View Scheme
参考文献
ARAGON PHARMACEUTICALS, INC.; SMITH, Nicholas, D.; BONNEFOUS, Celine; JULIEN, Jackaline, D.
Patent: WO2011/103202 A2, 2011 ;
WO 2011/103202 A2
反应条件
1: 1,1'-bis-(diphenylphosphino)ferrocene; tris-(dibenzylideneacetone)dipalladium(0) / N,N-dimethyl-formamide / 0.5 h / 170 °C / Reflux; Inert atmosphere
2: trifluoroacetic acid / dichloromethane / 3 h / 20 °C
View Scheme
参考文献
ARAGON PHARMACEUTICALS, INC.; SMITH, Nicholas, D.; BONNEFOUS, Celine; JULIEN, Jackaline, D.
Patent: WO2011/103202 A2, 2011 ;
WO 2011/103202 A2