2-((4-氯苯基磺酰基)甲基)-1,4-二氟苯合成路线 （共 15 条）
反应条件
1.1: 92 percent / acetic anhydride / dimethylformamide / 24.5 h / 60 °C
2.1: xylene / 16 h / 130 °C
3.1: 110 g / aq. HCl / xylene; tetrahydrofuran / 2 h / 50 °C
4.1: potassium tert-butoxide / tetrahydrofuran / 1 h / -5 °C
4.2: 97 percent / tetrahydrofuran / 20 h / 22 °C
5.1: 94 percent / L-selectride / tetrahydrofuran / 1.5 h / -60 °C
View Scheme
参考文献
Scott, Jeremy P.; Lieberman, David R.; Beureux, Olivier M.; Brands, Karel M. J.; Davies, Antony J.; Gibson, Andrew W.; Hammond, Deborah C.; McWilliams, Chris J.; Stewart, Gavin W.; Wilson, Robert D.; Dolling, Ulf-H.
Journal of Organic Chemistry, 2007 , vol. 72, # 11 p. 4149 - 4155
反应条件
bis-dimethylamino-methane in DMF (N,N-dimethyl-formamide)
T=60°C; 5 h;
参考文献
MERCK SHARP and DOHME LIMITED; MERCK and CO., INC.
Patent: WO2004/13090 A1, 2004 ;
Location in patent: Page 12 ;
反应条件
acetic anhydride in N,N-dimethyl-formamide
T=60°C; 24.5 h;
参考文献
Scott, Jeremy P.; Lieberman, David R.; Beureux, Olivier M.; Brands, Karel M. J.; Davies, Antony J.; Gibson, Andrew W.; Hammond, Deborah C.; McWilliams, Chris J.; Stewart, Gavin W.; Wilson, Robert D.; Dolling, Ulf-H.
Journal of Organic Chemistry, 2007 , vol. 72, # 11 p. 4149 - 4155
反应条件
acetic anhydride in N,N-dimethyl-formamide
T=60°C; 2.5 h;
参考文献
Scott, Jeremy P.; Lieberman, David R.; Beureux, Olivier M.; Brands, Karel M. J.; Davies, Antony J.; Gibson, Andrew W.; Hammond, Deborah C.; McWilliams, Chris J.; Stewart, Gavin W.; Wilson, Robert D.; Dolling, Ulf-H.
Journal of Organic Chemistry, 2007 , vol. 72, # 11 p. 4149 - 4155
反应条件
(tributylphosphoranylidene)acetonitrile in toluene
28 h; Heating / reflux;
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: EP1640366 A1, 2006 ;
Location in patent: Page/Page column 31-32 ;
