N-[4-氰基-3-(三氟甲基)苯基]甲基环氧丙烯酰胺合成路线 （共 18 条）
反应条件
1: N1-[4-cyano-3-(trifluoromethyl)phenyl]-(2R)-3-bromo-2-hydroxy-2-methylpropanamide With potassium carbonate in acetone 2 h; Reflux; 2: α-naphthol in isopropyl alcohol 18 h; Reflux;
参考文献
Journal of Medicinal Chemistry, , vol. 54, # 11 p. 3973 - 3976
反应条件
1: 4-fluorophenyl mercaptan; N-[4-cyano-3-(trifluoromethyl)phenyl]-2-methyl-2-oxiranecarboxamide With methanol; sodium hydroxide; water T=0 - 25°C; 3.5 h; 2: N-[4-cyano-3-(trifluoromethyl)phenyl]-2-methyl-2-oxiranecarboxamide With hydrogenchloride; water T=5°C; pH=< 7; 3 h;
参考文献
Apotex Pharmachem Inc.
Patent: US2007/27211 A1, 2007 ;
Location in patent: Page/Page column 2; 4 ;
反应条件
in toluene T=60 - 70°C; 2 h;
参考文献
SOLMAG S.p.A.
Patent: EP1777216 A1, 2007 ;
Location in patent: Page/Page column 5 ;
反应条件
in dimethyl sulfoxide T=50°C; pH=10; aq. buffer; Kinetics; pH-value;
参考文献
Asaad, Nabil; Fillery, Shaun
Organic and Biomolecular Chemistry, 2009 , vol. 7, # 4 p. 678 - 686
反应条件
1: With sodium hydroxide; tetra(n-butyl)ammonium hydrogensulfate in water; ethyl acetate T=25 - 30°C; 3 h; 2: With potassium permanganate in water; ethyl acetate 2.5 h; 3: With Na2S2O5 in water; ethyl acetate T=50°C; 1 h; Product distribution / selectivity;
参考文献
SUN PHARMACEUTICAL INDUSTRIES LIMITED
Patent: WO2007/13094 A2, 2007 ;
Location in patent: Page/Page column 10 ;
反应条件
tetrabutylammomium bromide in chloroform; water 96 h; Heating / reflux;
参考文献
Thijs, Lambertus; Keltjens, Rolf; Ettema, Gerrit J. B.
Patent: US2004/68135 A1, 2004 ;
Location in patent: Page 16 ;
反应条件
1: sodium hydride / tetrahydrofuran / 2 h / 20 °C 2: 255.2 g / hydrogen peroxide; trifluoroacetic anhydride / CH2Cl2 / 16 h / 20 °C View Scheme
参考文献
Tucker; Crook; Chesterson
Journal of Medicinal Chemistry, 1988 , vol. 31, # 5 p. 954 - 959
反应条件
in dimethyl sulfoxide T=50°C; pH=10; aq. buffer; Kinetics;
参考文献
Asaad, Nabil; Fillery, Shaun
Organic and Biomolecular Chemistry, 2009 , vol. 7, # 4 p. 678 - 686
