4-(4-氟苯甲酰基)-3-羟甲基 苯甲氰合成路线 (共 11 条)
反应条件
1: in tetrahydrofuran; ethylene glycol dimethyl ether T=-10°C; 3.5 h; 2: With water; ammonium chloride in tetrahydrofuran; ethylene glycol dimethyl ether T=20°C; 0.0833333 h;
参考文献
WO2007/82771 A1, ;
Page/Page column 22 ;
反应条件
in tetrahydrofuran; water T=-10 - -5°C; 3 h;
参考文献
WO2004/80988 A1, ;
Page 17-18; 13; 7; 20-21 ;
反应条件
1: 1-bromo-4-fluorobenzene With magnesium in tetrahydrofuran RefluxInert atmosphere; 2: 5-cyano-isobenzofuran-1-one in tetrahydrofuran T=0°C; 0.5 h; Inert atmosphere;
参考文献
Organic Process Research and Development, , vol. 16, # 5 p. 824 - 829
反应条件
1: 4-(4-fluorobenzoyl)-3-(hydroxymethyl)benzonitrile With methyl boronic acid in toluene T=20 - 70°C; 0.75 h; 2: 3-(N,N-dimethylamino)-propylmagnesium chloride in tetrahydrofuran; toluene T=-60°C; 0.2 h; Product distribution / selectivity;
参考文献
SANDOZ AG
Patent: WO2007/82771 A1, 2007 ;
Location in patent: Page/Page column 23 ;
反应条件
1: 4-(4-fluorobenzoyl)-3-(hydroxymethyl)benzonitrile With (1S,2R)-(+)-N-methylephedrine in toluene T=20 - 70°C; 0.75 h; 2: 3-(N,N-dimethylamino)-propylmagnesium chloride in tetrahydrofuran; toluene T=-80°C; 0.2 h; Product distribution / selectivity;
参考文献
SANDOZ AG
Patent: WO2007/82771 A1, 2007 ;
Location in patent: Page/Page column 21 ;
反应条件
1: 4-(4-fluorobenzoyl)-3-(hydroxymethyl)benzonitrile With (1S,2R)-(+)-N-methylephedrine in toluene T=20 - 70°C; 0.75 h; 2: 3-(N,N-dimethylamino)-propylmagnesium chloride in tetrahydrofuran; toluene T=-80°C; 0.2 h; Product distribution / selectivity;
参考文献
SANDOZ AG
Patent: WO2007/82771 A1, 2007 ;
Location in patent: Page/Page column 21 ;
反应条件
sodium tetrahydroborate in methanol; toluene T=10 - 15°C; 2 h;
参考文献
JUBILANT ORGANOSYS LIMITED
Patent: WO2005/77927 A1, 2005 ;
Location in patent: Page/Page column 8-9 ;
反应条件
1: With sodium hydroxide; sodium tetrahydroborate in tetrahydrofuran; water T=0 - 15°C; 0.5 h; 2: With phosphoric acid in water 2 h; Heating / reflux;
参考文献
ADORKEM TECHNOLOGY SPA
Patent: WO2004/80988 A1, 2004 ;
Location in patent: Page 18-19; 20-21; 13; 7 ;
反应条件
1: 4-(4-fluorobenzoyl)-3-(hydroxymethyl)benzonitrile With (1S,2R)-(+)-N-methylephedrine in toluene T=20 - 70°C; 0.75 h; 2: 3-(N,N-dimethylamino)-propylmagnesium chloride in tetrahydrofuran; toluene T=-80°C; 0.2 h; Product distribution / selectivity;
参考文献
SANDOZ AG
Patent: WO2007/82771 A1, 2007 ;
Location in patent: Page/Page column 21 ;
反应条件
in toluene T=20 - 70°C; P=45.0045 - 52.5053 Torr; 0.866667 - 1.03333 h; Product distribution / selectivity;
参考文献
SANDOZ AG
Patent: WO2007/82771 A1, 2007 ;
Location in patent: Page/Page column 16-18 ;