2-氨基-4,6-二氟苯甲酸合成路线 （共 25 条）
参考文献
Societe de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Patent: US6815546 B2, 2004 ;
反应条件
ammonia; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride in tetrahydrofuran; dioxanes; N,N-dimethyl acetamide
T=20°C; 24 h;
参考文献
SMITHKLINE BEECHAM CORPORATION
Patent: WO2009/20990 A1, 2009 ;
Location in patent: Page/Page column 72-73 ;
WO 2009/020990 A1
反应条件
triphenylphosphine; diethylazodicarboxylate in dichloromethane
T=20°C; Mitsunobu reaction; 1 h;
参考文献
Hennequin, Laurent F.; Allen, Jack; Breed, Jason; Curwen, Jon; Fennell, Michael; Green, Tim P.; Lambert-Van Der Brempt, Christine; Morgentin, Remy; Norman, Richard A.; Olivier, Annie; Otterbein, Ludovic; Ple, Patrick A.; Warin, Nicolas; Costello, Gerard
Journal of Medicinal Chemistry, 2006 , vol. 49, # 22 p. 6465 - 6488
反应条件
1: 3,5-difluoroanthranilic acid With 1-methyl-pyrrolidin-2-one in tert-butyl methyl ether
Large scale reaction;
2: With potassium carbonate in tert-butyl methyl ether
T=3°C; 1 h; Large scale reaction;
3: dimethyl sulfate in tert-butyl methyl ether
T=2°C; 2.58333 h; Large scale reaction;
参考文献
Ford, J. Gair; Pointon, Simon M.; Powell, Lyn; Siedlecki, Paul S.; Baum, John; Chubb, Richard; Fieldhouse, Robin; Muxworthy, James; Nivlet, Alex; Stenson, Rachel; Warwick, Eleanor
Organic Process Research and Development, 2010 , vol. 14, # 5 p. 1078 - 1087
反应条件
1.1: 1-methyl-pyrrolidin-2-one / tert-butyl methyl ether / Large scale reaction
1.2: 1 h / 3 °C / Large scale reaction
1.3: 2.58 h / 2 °C / Large scale reaction
2.1: N-ethyl-N,N-diisopropylamine / V methoxymethyl ester; toluene / 40 - 123 °C / Large scale reaction
3.1: sodium hydride / N,N-dimethyl acetamide / 1 h / 17 - 22 °C / Large scale reaction
3.2: 17 h / 11 - 90 °C / Large scale reaction
View Scheme
参考文献
Ford, J. Gair; Pointon, Simon M.; Powell, Lyn; Siedlecki, Paul S.; Baum, John; Chubb, Richard; Fieldhouse, Robin; Muxworthy, James; Nivlet, Alex; Stenson, Rachel; Warwick, Eleanor
Organic Process Research and Development, 2010 , vol. 14, # 5 p. 1078 - 1087
