6-氟-1H-吲唑-5-甲腈(9ci)合成路线 （共 5 条）
反应条件
1: With tetrakis(triphenylphosphine) palladium(0) in N,N-dimethyl-formamide
T=120 - 130°C; 36 h; Inert atmosphere;
2: With water; sodium hydrogencarbonate in ethyl acetate
参考文献
GLAXO GROUP LIMITED; BAILEY, James; KING, Nigel Paul; LIN, Xichen; REN, Feng; TAN, Kheng-Chuan; MAK, Sing Yeung
Patent: WO2011/72488 A1, 2011 ;
Location in patent: Page/Page column 17; 39 ;
WO 2011/072488 A1
反应条件
tetrakis(triphenylphosphine) palladium(0) in N,N-dimethyl-formamide
T=115°C; 90 h; Inert atmosphere;
参考文献
GLAXO GROUP LIMITED; BAILEY, James; KING, Nigel Paul; LIN, Xichen; REN, Feng; TAN, Kheng-Chuan; MAK, Sing Yeung
Patent: WO2011/72488 A1, 2011 ;
Location in patent: Page/Page column 17; 39-40 ;
WO 2011/072488 A1
反应条件
pyridine; hydrazine
T=20°C; 2 h;
参考文献
Eisai Co., Ltd.
Patent: EP1510516 A1, 2005 ;
Location in patent: Page/Page column 85 ;
反应条件
1.1: chloroform / 20 °C / Cooling with ice
1.2: 16 h / 75 °C
2.1: tetrakis(triphenylphosphine) palladium(0) / N,N-dimethyl-formamide / 36 h / 120 - 130 °C / Inert atmosphere
View Scheme
参考文献
GLAXO GROUP LIMITED; BAILEY, James; KING, Nigel Paul; LIN, Xichen; REN, Feng; TAN, Kheng-Chuan; MAK, Sing Yeung
Patent: WO2011/72488 A1, 2011 ;
WO 2011/072488 A1
反应条件
1: tetrakis(triphenylphosphine) palladium(0) / N,N-dimethyl-formamide / 36 h / 120 - 130 °C / Inert atmosphere
2: tetrakis(triphenylphosphine) palladium(0) / N,N-dimethyl-formamide / 90 h / 115 °C / Inert atmosphere
View Scheme
参考文献
GLAXO GROUP LIMITED; BAILEY, James; KING, Nigel Paul; LIN, Xichen; REN, Feng; TAN, Kheng-Chuan; MAK, Sing Yeung
Patent: WO2011/72488 A1, 2011 ;
WO 2011/072488 A1
