2-(4-氟苯基)-5-羟基-3-苯并呋喃羧酸乙酯合成路线 （共 7 条）
反应条件
zinc(II) chloride in tetrahydrofuran; toluene
6 h; RefluxInert atmosphere;
参考文献
ABBOTT LABORATORIES; ABBOTT GMBH and CO.KG; MARING, Clarence J.; PRATT, John K.; CARROLL, William A.; LIU, Dachun; BETEBENNER, David A.; HUTCHINSON, Douglas K.; TUFANO, Michael D.; ROCKWAY, Todd W.; SCHOEN, Uwe; PAHL, Axel; WITTE, Adreas
Patent: WO2012/87833 A1, 2012 ;
Location in patent: Page/Page column 120 ;
WO 2012/087833 A1
反应条件
1.1: potassium tert-butylate / toluene / 78 °C / Inert atmosphere
1.2: 78 °C / Inert atmosphere
1.3: 78 °C / Inert atmosphere
2.1: zinc(II) chloride / toluene; tetrahydrofuran / 6 h / Reflux; Inert atmosphere
View Scheme
参考文献
ABBOTT LABORATORIES; ABBOTT GMBH and CO.KG; MARING, Clarence J.; PRATT, John K.; CARROLL, William A.; LIU, Dachun; BETEBENNER, David A.; HUTCHINSON, Douglas K.; TUFANO, Michael D.; ROCKWAY, Todd W.; SCHOEN, Uwe; PAHL, Axel; WITTE, Adreas
Patent: WO2012/87833 A1, 2012 ;
WO 2012/087833 A1
反应条件
1-methyl-pyrrolidin-2-one; caesium carbonate
T=50°C; 4 h; Inert atmosphere;
参考文献
ABBOTT LABORATORIES; ABBOTT GMBH and CO.KG; MARING, Clarence J.; PRATT, John K.; CARROLL, William A.; LIU, Dachun; BETEBENNER, David A.; HUTCHINSON, Douglas K.; TUFANO, Michael D.; ROCKWAY, Todd W.; SCHOEN, Uwe; PAHL, Axel; WITTE, Adreas
Patent: WO2012/87833 A1, 2012 ;
Location in patent: Page/Page column 120 ;
WO 2012/087833 A1
反应条件
1: 1-methyl-pyrrolidin-2-one; caesium carbonate / 4 h / 50 °C / Inert atmosphere
2: nitric acid / chloroform / 1 h / 0 - 20 °C
View Scheme
参考文献
ABBOTT LABORATORIES; ABBOTT GMBH and CO.KG; MARING, Clarence J.; PRATT, John K.; CARROLL, William A.; LIU, Dachun; BETEBENNER, David A.; HUTCHINSON, Douglas K.; TUFANO, Michael D.; ROCKWAY, Todd W.; SCHOEN, Uwe; PAHL, Axel; WITTE, Adreas
Patent: WO2012/87833 A1, 2012 ;
WO 2012/087833 A1
反应条件
nitric acid in chloroform
T=-20°C; 0.166667 h;
参考文献
BRISTOL-MYERS SQUIBB COMPANY; YEUNG, Kap-Sun; PARCELLA, Kyle, E.; BENDER, John, A.; BENO, Brett, R.; GRANT-YOUNG, Katharine, A.; HAN, Ying; HEWAWASAM, Piyasena; KADOW, John, F.; NICKEL, Andrew
Patent: WO2011/112191 A1, 2011 ;
Location in patent: Page/Page column 166-167 ;
WO 2011/112191 A1
反应条件
1.1: 1-methyl-pyrrolidin-2-one; caesium carbonate / 4 h / 50 °C / Inert atmosphere
2.1: nitric acid / chloroform / 1 h / 0 - 20 °C
3.1: boron trichloride / dichloromethane / 1 h / 0 - 20 °C
3.2: 20 °C
View Scheme
参考文献
ABBOTT LABORATORIES; ABBOTT GMBH and CO.KG; MARING, Clarence J.; PRATT, John K.; CARROLL, William A.; LIU, Dachun; BETEBENNER, David A.; HUTCHINSON, Douglas K.; TUFANO, Michael D.; ROCKWAY, Todd W.; SCHOEN, Uwe; PAHL, Axel; WITTE, Adreas
Patent: WO2012/87833 A1, 2012 ;
WO 2012/087833 A1
反应条件
1.1: 1-methyl-pyrrolidin-2-one; caesium carbonate / 4 h / 50 °C / Inert atmosphere
2.1: nitric acid / chloroform / 1 h / 0 - 20 °C
3.1: boron trichloride / dichloromethane / 1 h / 0 - 20 °C
3.2: 20 °C
4.1: 4-(N,N-dimethlyamino)pyridine; N-ethyl-N,N-diisopropylamine / dichloromethane / 18 h
5.1: sodium bromide; KF*2H2O / tetrakis(triphenylphosphine) palladium(0) / toluene / 18 h / 125 °C / Inert atmosphere; sealed vessel
6.1: ammonium chloride; iron / ethanol; water; tetrahydrofuran / 1.5 h / Inert atmosphere; Reflux
View Scheme
参考文献
ABBOTT LABORATORIES; ABBOTT GMBH and CO.KG; MARING, Clarence J.; PRATT, John K.; CARROLL, William A.; LIU, Dachun; BETEBENNER, David A.; HUTCHINSON, Douglas K.; TUFANO, Michael D.; ROCKWAY, Todd W.; SCHOEN, Uwe; PAHL, Axel; WITTE, Adreas
Patent: WO2012/87833 A1, 2012 ;
WO 2012/087833 A1
