2-羟基-3-[5-(吗啉-4-甲基)吡啶-2-基]-1H-吲哚-5-甲腈合成路线 (共 5 条)
反应条件
1: 5-bromo-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]-1H-indol-2-ol With zinc; tri-tert-butyl phosphine; bis(dibenzylideneacetone)-palladium(0) in N,N-dimethyl-formamide
T=50°C; 0.0666667 h;
2: zinc cyanide in N,N-dimethyl-formamide
T=50°C; 3 h; Product distribution / selectivity;
参考文献
ASTRAZENECA AB
Patent: WO2007/89193 A1, 2007 ;
Location in patent: Page/Page column 23-24 ;
WO 2007/089193 A1
反应条件
1: With iron; acetic acid
T=60°C; 3 h;
2: With ammonia in methanol; dichloromethane
Product distribution / selectivity;
参考文献
ASTRAZENECA AB
Patent: WO2008/130312 A1, 2008 ;
Location in patent: Page/Page column 37 ;
WO 2008/130312 A1
反应条件
triethylamine in acetic acid n-butyl ester
T=90°C; Product distribution / selectivity;
参考文献
ASTRAZENECA AB
Patent: WO2008/130312 A1, 2008 ;
Location in patent: Page/Page column 36 ;
WO 2008/130312 A1
反应条件
1: 2-oxo-2,3-dihydro-indole-5-carbonitrile With sodium hydride in N,N-dimethyl-formamide
0.25 h;
2: N-(6-chloropyridin-3-ylmethyl)morpholine in N,N-dimethyl-formamide
1 h; Heating / reflux; Product distribution / selectivity;
参考文献
ASTRAZENECA AB
Patent: WO2003/82853 A1, 2003 ;
Location in patent: Page/Page column 59 ;
WO 03/082853 A1
反应条件
[(t-Bu3P)PdBr]2; zinc in N,N-dimethyl-formamide
T=40 - 50°C; 3 h; Inert atmosphereSchlenk techniqueLarge scale; Reagent/catalyst;
参考文献
Ryberg, Per
Organic Process Research and Development, 2008 , vol. 12, # 3 p. 540 - 543