1.1: methyl-magnesium chloride / tert-butyl methyl ether; tetrahydrofuran / 0.75 h / 20 °C 1.2: 0.5 h / 3 - 20 °C 2.1: lithium aluminium tetrahydride / tetrahydrofuran / 3.5 h / 60 °C / Reflux 3.1: isopropyl alcohol; water / 4 h / 20 - 35 °C 4.1: potassium hydroxide / toluene; water / 0.25 h / 21 - 25 °C 4.2: 4 h / 100 °C View Scheme

ammonia in N,N-dimethyl-formamide T=0 - 20°C; 16.16 h; Product distribution / selectivity;

1.1: methyl-magnesium chloride / tert-butyl methyl ether; tetrahydrofuran / 0.75 h / 20 °C 1.2: 0.5 h / 3 - 20 °C 2.1: lithium aluminium tetrahydride / tetrahydrofuran / 3.5 h / 60 °C / Reflux View Scheme

1.1: ethylmagnesium bromide / dichloromethane; diethyl ether / 0.5 h / Reflux 1.2: 10 h / -25 - -15 °C 2.1: lithium aluminium tetrahydride / tetrahydrofuran / 0 °C / Reflux 2.2: 0 - 5 °C View Scheme

1: 5-Bromo-1H-indole With ethylmagnesium bromide in tetrahydrofuran T=0°C; 0.5 h; 2: N-(benzyloxycarbonyl)-D-proline, acid chloride in tetrahydrofuran T=0°C; 1.5 h;

1: 5-Bromo-1H-indole; N-(benzyloxycarbonyl)-D-proline, acid chloride With 1,1-dimethylethylmagnesium chloride in diethyl ether T=0 - 20°C; 0.75 h; 2: sodium hydrogencarbonate in diethyl ether; water; ethyl acetate

1: 5-Bromo-1H-indole; methyl-magnesium chloride in tetrahydrofuran; tert-butyl methyl ether T=20°C; 0.75 h; 2: N-(benzyloxycarbonyl)-D-proline, acid chloride in tetrahydrofuran; tert-butyl methyl ether T=3 - 20°C; 0.5 h; 3: With citric acid in tetrahydrofuran; tert-butyl methyl ether; water pH=3;

ammonium chloride in dichloromethane; water; N,N-dimethyl-formamide; toluene

暂无反应条件数据

1.1: methyl-magnesium chloride / tert-butyl methyl ether; tetrahydrofuran / 0.75 h / 20 °C 1.2: 0.5 h / 3 - 20 °C 2.1: lithium aluminium tetrahydride / tetrahydrofuran / 3.5 h / 60 °C / Reflux 3.1: isopropyl alcohol; water / 4 h / 20 - 35 °C 4.1: potassium hydroxide / toluene; water / 0.25 h / 21 - 25 °C 4.2: 4 h / 100 °C 5.1: triethylamine / palladium diacetate; tris-(o-tolyl)phosphine / N,N-dimethyl-formamide / 5 h / 115 °C 6.1: potassium carbonate; water / methanol 7.1: hydrogen bromide / water / pH 1.5 8.1: hydrogen / 5 Pd(II)/C(eggshell) / water / 20 - 50 °C / Autoclave View Scheme