(3R,4R)-3-(5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉)-4-(1H-吲哚)-2,5-吡咯烷二酮合成路线 (共 5 条)
反应条件
hydrogenchloride in 3-methyl-tetrahydrofuran; water T=50°C; pH=1.6; Product distribution / selectivity;
参考文献
US2011/160242 A1, ;
Page/Page column 27-29 ;
反应条件
1.1: tert-butyl methyl ether / 2.17 h / 15 - 32 °C / Industry scale 1.2: 2 h / Industry scale 2.1: potassium tert-butylate / tetrahydrofuran / 3 h / 20 - 32 °C / Industry scale 2.2: 0.5 h / 40 - 50 °C / Industry scale 2.3: 40 °C / pH 8 - 9 / Industry scale 3.1: hydrogen; potassium tert-butylate / Pearlman's catalist / tetrahydrofuran / 45 - 55 °C / 3361.55 - 4137.29 Torr / Industry scale 4.1: hydrogenchloride / water; isopropanol acetate / Industry scale 5.1: Chiralpak AZ column / dichloromethane; acetonitrile; methanol / Resolution of racemate; Multicolumn chromatography View Scheme
反应条件
1.1: potassium tert-butylate / tetrahydrofuran / 3 h / 20 - 32 °C / Industry scale 1.2: 0.5 h / 40 - 50 °C / Industry scale 1.3: 40 °C / pH 8 - 9 / Industry scale 2.1: hydrogen; potassium tert-butylate / Pearlman's catalist / tetrahydrofuran / 45 - 55 °C / 3361.55 - 4137.29 Torr / Industry scale 3.1: hydrogenchloride / water; isopropanol acetate / Industry scale 4.1: Chiralpak AZ column / dichloromethane; acetonitrile; methanol / Resolution of racemate; Multicolumn chromatography View Scheme
反应条件
1: hydrogen; potassium tert-butylate / Pearlman's catalist / tetrahydrofuran / 45 - 55 °C / 3361.55 - 4137.29 Torr / Industry scale 2: hydrogenchloride / water; isopropanol acetate / Industry scale 3: Chiralpak AZ column / dichloromethane; acetonitrile; methanol / Resolution of racemate; Multicolumn chromatography View Scheme
反应条件
1.1: sodium hydroxide / ethanol / 13 h / 65 °C / Industry scale 1.2: 60 °C 2.1: acetonitrile / 50 °C 3.1: hydrogenchloride / 3-methyl-tetrahydrofuran; water / 50 °C / pH 1.6 View Scheme