1: 4-methoxy-aniline With boron trichloride in dichloromethane; chlorobenzene
T=20°C; 1 h;
2: m-fluorobenzene nitrile With AlCl3, aluminium chloride in dichloromethane; chlorobenzene
T=60 - 70°C; 3 h;
3: With water in dichloromethane; chlorobenzene
T=85°C; 6 h; Product distribution / selectivity;
参考文献
MERCK and CO., INC.
Patent: WO2005/30129 A2, 2005 ;
Location in patent: Page/Page column 22; 31-32 ;
WO 2005/030129 A2
n-butyllithium in tetrahydrofuran; hexane
T=-78°C; Inert atmosphere;
参考文献
Acker, Timothy M.; Khatri, Alpa; Vance, Katie M.; Slabber, Cathryn; Bacsa, John; Snyder, James P.; Traynelis, Stephen F.; Liotta, Dennis C.
Journal of Medicinal Chemistry, 2013 , vol. 56, # 16 p. 6434 - 6456
1.1: tetrahydrofuran / 2 h / 70 °C
2.1: triethylamine / ethanol / 0.17 h
2.2: 2 h / |Reflux
3.1: n-butyllithium / tetrahydrofuran; hexane / -78 °C / |Inert atmosphere
View Scheme
参考文献
Acker, Timothy M.; Khatri, Alpa; Vance, Katie M.; Slabber, Cathryn; Bacsa, John; Snyder, James P.; Traynelis, Stephen F.; Liotta, Dennis C.
Journal of Medicinal Chemistry, 2013 , vol. 56, # 16 p. 6434 - 6456
1.1: triethylamine / ethanol / 0.17 h
1.2: 2 h / |Reflux
2.1: n-butyllithium / tetrahydrofuran; hexane / -78 °C / |Inert atmosphere
View Scheme
参考文献
Acker, Timothy M.; Khatri, Alpa; Vance, Katie M.; Slabber, Cathryn; Bacsa, John; Snyder, James P.; Traynelis, Stephen F.; Liotta, Dennis C.
Journal of Medicinal Chemistry, 2013 , vol. 56, # 16 p. 6434 - 6456
