2-氯-N-苯基-4-吡啶羧酰胺合成路线 （共 9 条）
反应条件
in methanol 16 h; Heating;
参考文献
Epsztajn, Jan; Bieniek, Adam; Plotka, Mieczyslaw W.; Suwald, Krzysztof
Tetrahedron, 1989 , vol. 45, # 23 p. 7469 - 7476
反应条件
1: With n-butyllithium in tetrahydrofuran; hexane T=-78°C; 0.5 h; 2: With methyl iodide in tetrahydrofuran; hexane T=-78 - 33°C; 1.5 h;
参考文献
ACTELION PHARMACEUTICALS LTD
Patent: WO2005/54244 A2, 2005 ;
Location in patent: Page/Page column 23 ;
反应条件
1: 2-chloro-N-phenylisonicotinamide With n-butyllithium in tetrahydrofuran; hexanes T=-78°C; 1.23333 h; Inert atmosphere; 2: methyl iodide in tetrahydrofuran; hexanes T=-78 - 20°C; 21.1333 h;
参考文献
EPIZYME, INC.; EISAI CO., LTD.; KUNTZ, Kevin, Wayne; CHESWORTH, Richard; DUNCAN, Kenneth, William; KEILHACK, Heike; WARHOLIC, Natalie; KLAUS, Christine; ZHENG, Wanjun
Patent: WO2012/142513 A1, 2012 ;
Location in patent: Page/Page column 427 ;
WO 2012/142513 A1
反应条件
N-ethyl-N,N-diisopropylamine in 1,2-dichloro-ethane
T=0 - 95°C; 2 h;
参考文献
ACTELION PHARMACEUTICALS LTD
Patent: WO2005/40173 A1, 2005 ;
Location in patent: Page/Page column 33-34 ;
反应条件
phosphorus pentachloride in trichlorophosphate
T=130°C; 1.5 h;
参考文献
Epsztajn, Jan; Bieniek, Adam; Plotka, Mieczyslaw W.; Suwald, Krzysztof
Tetrahedron, 1989 , vol. 45, # 23 p. 7469 - 7476
反应条件
1.1: thionyl chloride / N,N-dimethyl-formamide / toluene / 71.67 h / 20 - 100 °C / Inert atmosphere
2.1: N-ethyl-N,N-diisopropylamine / 19 h / Inert atmosphere
2.2: 35 h
View Scheme
参考文献
EPIZYME, INC.; EISAI CO., LTD.; KUNTZ, Kevin, Wayne; CHESWORTH, Richard; DUNCAN, Kenneth, William; KEILHACK, Heike; WARHOLIC, Natalie; KLAUS, Christine; ZHENG, Wanjun
Patent: WO2012/142513 A1, 2012 ;
WO 2012/142513 A1
反应条件
1: SOCl
2: Et3N / CHCl3
3: 81 percent / hydrogen peroxide / acetic acid / 10 h / 85 °C
4: 65 percent / phosphorus pentachloride / POCl3 / 1.5 h / 130 °C
View Scheme
参考文献
Epsztajn, Jan; Bieniek, Adam; Plotka, Mieczyslaw W.; Suwald, Krzysztof
Tetrahedron, 1989 , vol. 45, # 23 p. 7469 - 7476
反应条件
1: Et3N / CHCl3
2: 81 percent / hydrogen peroxide / acetic acid / 10 h / 85 °C
3: 65 percent / phosphorus pentachloride / POCl3 / 1.5 h / 130 °C
View Scheme
参考文献
Epsztajn, Jan; Bieniek, Adam; Plotka, Mieczyslaw W.; Suwald, Krzysztof
Tetrahedron, 1989 , vol. 45, # 23 p. 7469 - 7476
反应条件
1: 81 percent / hydrogen peroxide / acetic acid / 10 h / 85 °C
2: 65 percent / phosphorus pentachloride / POCl3 / 1.5 h / 130 °C
View Scheme
参考文献
Epsztajn, Jan; Bieniek, Adam; Plotka, Mieczyslaw W.; Suwald, Krzysztof
Tetrahedron, 1989 , vol. 45, # 23 p. 7469 - 7476
