5-[(2R)-2-氨基丙基]-1-[3-(苯甲酰氧基)丙基]-2,3-二氢-7-氰基-1H-吲哚酒石酸盐合成路线 （共 11 条）
反应条件
in water; acetone T=25 - 65°C; Resolution of racemate;
参考文献
WO2013/56842 A1, ;
Page/Page column 19; 20 ;
反应条件
in tetrahydrofuran; water T=20 - 65°C; Product distribution / selectivity;
参考文献
WO2012/131710 A2, ;
Page/Page column 32-33 ;
反应条件
1: hydrogenchloride; zinc / water; methanol / 20 h / 60 - 65 °C 2: water; tetrahydrofuran / 20 - 65 °C View Scheme
反应条件
1.1: sodium tetrahydroborate; potassium hydroxide / tetrahydrofuran; water / -10 - 20 °C 2.1: trichlorophosphate / 0 - 50 °C 2.2: |Cooling with ice 3.1: hydroxylamine hydrochloride; pyridine / tetrahydrofuran / 2 h / 50 °C 3.2: 2 h / 80 °C 4.1: platinum on carbon; hydrogen / ethyl acetate / 25 - 30 °C / 6000.6 - 7500.75 Torr / |Autoclave 5.1: acetone; water / 25 - 65 °C / |Resolution of racemate View Scheme
反应条件
1.1: trichlorophosphate / 0 - 50 °C 1.2: |Cooling with ice 2.1: hydroxylamine hydrochloride; pyridine / tetrahydrofuran / 2 h / 50 °C 2.2: 2 h / 80 °C 3.1: platinum on carbon; hydrogen / ethyl acetate / 25 - 30 °C / 6000.6 - 7500.75 Torr / |Autoclave 4.1: acetone; water / 25 - 65 °C / |Resolution of racemate View Scheme
反应条件
1.1: hydroxylamine hydrochloride; pyridine / tetrahydrofuran / 2 h / 50 °C 1.2: 2 h / 80 °C 2.1: platinum on carbon; hydrogen / ethyl acetate / 25 - 30 °C / 6000.6 - 7500.75 Torr / |Autoclave 3.1: acetone; water / 25 - 65 °C / |Resolution of racemate View Scheme
反应条件
1: platinum on carbon; hydrogen / ethyl acetate / 25 - 30 °C / 6000.6 - 7500.75 Torr / |Autoclave 2: acetone; water / 25 - 65 °C / |Resolution of racemate View Scheme
反应条件
1.1: triethylamine / N,N-dimethyl-formamide / 20 °C 1.2: 3 h / 100 °C 2.1: trichlorophosphate / 2 h / 20 °C 2.2: |Cooling with ice 3.1: ammonium acetate / 20 - 100 °C 4.1: sodium tetrahydroborate; potassium hydroxide / tetrahydrofuran; water / -10 - 20 °C 5.1: trichlorophosphate / 0 - 50 °C 5.2: |Cooling with ice 6.1: hydroxylamine hydrochloride; pyridine / tetrahydrofuran / 2 h / 50 °C 6.2: 2 h / 80 °C 7.1: platinum on carbon; hydrogen / ethyl acetate / 25 - 30 °C / 6000.6 - 7500.75 Torr / |Autoclave 8.1: acetone; water / 25 - 65 °C / |Resolution of racemate View Scheme
反应条件
1.1: triethylamine / N,N-dimethyl-formamide / 20 °C 1.2: 3 h / 100 °C 2.1: trichlorophosphate / 2 h / 20 °C 2.2: |Cooling with ice 3.1: ammonium acetate / 20 - 100 °C 4.1: sodium tetrahydroborate; potassium hydroxide / tetrahydrofuran; water / -10 - 20 °C 5.1: trichlorophosphate / 0 - 50 °C 5.2: |Cooling with ice 6.1: hydroxylamine hydrochloride; pyridine / tetrahydrofuran / 2 h / 50 °C 6.2: 2 h / 80 °C 7.1: platinum on carbon; hydrogen / ethyl acetate / 25 - 30 °C / 6000.6 - 7500.75 Torr / |Autoclave 8.1: acetone; water / 25 - 65 °C / |Resolution of racemate View Scheme
反应条件
1.1: trichlorophosphate / 2 h / 20 °C 1.2: |Cooling with ice 2.1: ammonium acetate / 20 - 100 °C 3.1: sodium tetrahydroborate; potassium hydroxide / tetrahydrofuran; water / -10 - 20 °C 4.1: trichlorophosphate / 0 - 50 °C 4.2: |Cooling with ice 5.1: hydroxylamine hydrochloride; pyridine / tetrahydrofuran / 2 h / 50 °C 5.2: 2 h / 80 °C 6.1: platinum on carbon; hydrogen / ethyl acetate / 25 - 30 °C / 6000.6 - 7500.75 Torr / |Autoclave 7.1: acetone; water / 25 - 65 °C / |Resolution of racemate View Scheme
