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 6.1: 96 percent / diisobutylaluminium hydride / toluene / 1 h / -40 °C 7.1: potassium tert-butoxide / tetrahydrofuran / cooling 7.2: tetrahydrofuran; toluene / -20 - 20 °C 8.1: 5.6 kg / aq. HCl / tetrahydrofuran; toluene; dimethylformamide / 2 h / 45 °C 9.1: 74 percent / sulfamic acid; sodium chlorite / CH2Cl2; H2O / 0.5 h View Scheme
参考文献
Journal of Organic Chemistry, , vol. 72, # 11 p. 4149 - 4155
反应条件
sodium tungstate; sulfuric acid; dihydrogen peroxide; Aliquatreg; 336 in water; toluene
T=45°C;
参考文献
MERCK SHARP and DOHME LIMITED; MERCK and CO., INC.
Patent: WO2004/13090 A1, 2004 ;
Location in patent: Page 11-12 ;
反应条件
sulfuric acid; dihydrogen peroxide in n-heptane; water; toluene
参考文献
Churcher, Ian; Dinnell, Kevin; Harrison, Timothy; Kerrad, Sonia; Nadin, Alan John; Oakley, Paul Joseph; Shaw, Duncan Edward; Teall, Martin Richard; Williams, Susannah; Williams, Brian John
Patent: US2003/114496 A1, 2003 ;
反应条件
hexaammonium heptamolybdate tetrahydrate; dihydrogen peroxide in butan-1-ol
5 h; Heating / reflux;
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: EP1466898 A1, 2004 ;
Location in patent: Page 20; 21 ;
反应条件
1: 100 percent / sodium hydroxide / ethanol / cooling
2: 96 percent / sodium tungstate dihydrate; sulfuric acid; hydrogen peroxide / aliquat 336 / H2O; toluene / 45 °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
1: 100 percent / sodium hydroxide / ethanol / cooling
2: 96 percent / sodium tungstate dihydrate; sulfuric acid; hydrogen peroxide / aliquat 336 / H2O; toluene / 45 °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
in dichloromethane
2 h;
参考文献
MERCK SHARP & DOHME
Patent: JP2005/501120 A, 2005 ;
Location in patent: Page/Page column 12 ;
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
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
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
6.1: 96 percent / diisobutylaluminium hydride / toluene / 1 h / -40 °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
1: 92 percent / acetic anhydride / dimethylformamide / 24.5 h / 60 °C
2: xylene / 16 h / 130 °C
3: 110 g / aq. HCl / xylene; tetrahydrofuran / 2 h / 50 °C
View Scheme
参考文献
Teall, Martin; Oakley, Paul; Harrison, Timothy; Shaw, Duncan; Kay, Euan; Elliott, Jason; Gerhard, Ute; Castro, Jose L.; Shearman, Mark; Ball, Richard G.; Tsou, Nancy N.
Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 10 p. 2685 - 2688
