2-脱氧-2,2-二氟-D-赤型-戊糖酸-3,5-二苯甲酸-γ-内酯合成路线 （共 11 条）
反应条件
pyridine in ethyl acetate T=25 - 60°C; Inert atmosphere;
参考文献
WO2010/49947 A2, ;
Page/Page column 13 ;
反应条件
4-(N,N-dimethlyamino)pyridine in ethyl acetate T=60 - 65°C; 6.25 h;
参考文献
US2007/191598 A1, ;
Page/Page column 13 ;
反应条件
1: ethyl (3RS)-2,2-difluoro-3-(2,2-dimethyldioxolan-4-yl)propionate With water; pyridinium trifluoroacetate in water; acetonitrile 3 h; Heating / reflux; 2: benzoyl chloride With pyridine; 4-(N,N-dimethlyamino)pyridine in ethyl acetate T=0 - 65°C; 10 h; Product distribution / selectivity;
参考文献
WO2007/49295 A2, ;
Page/Page column 13; 15-16 ;
反应条件
1: ethyl 2-deoxy-2,2-difluoro-D-erythro,D-threo-pentonate With toluene-4-sulfonic acid in water T=75 - 80°C; 3 h; 2: benzoyl chloride With pyridine; 4-(N,N-dimethlyamino)pyridine in ethyl acetate T=60 - 65°C; 3 h; Dean and Stark apparatus; Product distribution / selectivity;
参考文献
WO2005/95430 A1, ;
Page/Page column 16 ;
反应条件
pyridine; 4-(N,N-dimethlyamino)pyridine in ethyl acetate T=60 - 65°C; 6 h; Product distribution / selectivity;
参考文献
WO2005/95430 A1, ;
Page/Page column 7; 13; 15 ;
反应条件
toluene-4-sulfonic acid in toluene Heating / refluxDean and Stark apparatus; Product distribution / selectivity;
参考文献
WO2005/95430 A1, ;
Page/Page column 15 ;
反应条件
1: 100 percent / LiAl(OBu-t)3H / diethyl ether; tetrahydrofuran / 1 h / 10 - 30 °C 2: 100 percent / triethylamine / CH2Cl2 / 2 h / 23 °C View Scheme
参考文献
ALIOS BIOPHARMA, INC.; Beigelman, Leonid; Wang, Guangyi; Smith, David Bernard; Deval, Jerome; Prhavc, Marija
Patent: US2013/165400 A1, 2013 ;
反应条件
1: 100 percent / LiAl(OBu-t)3H / diethyl ether; tetrahydrofuran / 1 h / 10 - 30 °C 2: 100 percent / triethylamine / CH2Cl2 / 2 h / 23 °C View Scheme
参考文献
ALIOS BIOPHARMA, INC.; Beigelman, Leonid; Wang, Guangyi; Smith, David Bernard; Deval, Jerome; Prhavc, Marija
Patent: US2013/165400 A1, 2013 ;
反应条件
1: 100 percent / LiAl(OBu-t)3H / diethyl ether; tetrahydrofuran / 1 h / 10 - 30 °C 2: 100 percent / triethylamine / CH2Cl2 / 2 h / 23 °C 3: 1) Me3SiOTf / 1) 1,1,2-trichloroethane, r.t., 30 min, 2) 113 deg C, 18 h View Scheme
参考文献
Chou; Heath; Patterson; Poteet; Lakin; Hunt
Synthesis, 1992 , # 6 p. 565 - 570
反应条件
1: 100 percent / LiAl(OBu-t)3H / diethyl ether; tetrahydrofuran / 1 h / 10 - 30 °C 2: 100 percent / triethylamine / CH2Cl2 / 2 h / 23 °C 3: 1) Me3SiOTf / 1) 1,1,2-trichloroethane, r.t., 30 min, 2) 113 deg C, 18 h View Scheme
参考文献
Chou; Heath; Patterson; Poteet; Lakin; Hunt
Synthesis, 1992 , # 6 p. 565 - 570
