Technology Process of N-({(4aS,R)-3-[(4'-chloro-[1,1'-biphenyl]-2-yl)methyl]-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinolin-8-yl}carbonyl)-4-({(1R)-3-(dimethylamino)-1-[(phenyl-sulphanyl)methyl]propyl}amino)-3-nitrobenzenesulphonamide
There total 12 articles about N-({(4aS,R)-3-[(4'-chloro-[1,1'-biphenyl]-2-yl)methyl]-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinolin-8-yl}carbonyl)-4-({(1R)-3-(dimethylamino)-1-[(phenyl-sulphanyl)methyl]propyl}amino)-3-nitrobenzenesulphonamide which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine;
In
tetrahydrofuran; dichloromethane;
at 20 ℃;
for 48h;
- Guidance literature:
-
Multi-step reaction with 8 steps
1.1: potassium carbonate; sodium iodide / N,N-dimethyl-formamide / 2 h / 80 °C
2.1: boron tribromide / dichloromethane / 0 - 20 °C
2.2: 0.5 h / 0 - 20 °C
3.1: triethylamine / dichloromethane
4.1: triethylamine / 1,1'-bis-(diphenylphosphino)ferrocene; palladium diacetate / dimethyl sulfoxide / 3.75 h / 65 °C
5.1: ammonium formate / palladium 10% on activated carbon / tetrahydrofuran; methanol / 4 h / 50 °C
6.1: potassium carbonate; sodium iodide / N,N-dimethyl-formamide / 2 h / 80 °C
7.1: hydrogenchloride; water / 1,4-dioxane / 4 h / Heating / reflux
8.1: dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine / tetrahydrofuran; dichloromethane / 48 h / 20 °C
With
hydrogenchloride; dmap; water; ammonium formate; boron tribromide; potassium carbonate; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; N-ethyl-N,N-diisopropylamine; sodium iodide;
1,1'-bis-(diphenylphosphino)ferrocene; palladium diacetate; palladium 10% on activated carbon;
In
tetrahydrofuran; 1,4-dioxane; methanol; dichloromethane; dimethyl sulfoxide; N,N-dimethyl-formamide;
- Guidance literature:
-
Multi-step reaction with 10 steps
1.1: potassium hydroxide / nickel / methanol; water / 20 °C
2.1: phosphorus pentoxide / o-xylene / 150 °C
3.1: potassium carbonate; sodium iodide / N,N-dimethyl-formamide / 2 h / 80 °C
4.1: boron tribromide / dichloromethane / 0 - 20 °C
4.2: 0.5 h / 0 - 20 °C
5.1: triethylamine / dichloromethane
6.1: triethylamine / 1,1'-bis-(diphenylphosphino)ferrocene; palladium diacetate / dimethyl sulfoxide / 3.75 h / 65 °C
7.1: ammonium formate / palladium 10% on activated carbon / tetrahydrofuran; methanol / 4 h / 50 °C
8.1: potassium carbonate; sodium iodide / N,N-dimethyl-formamide / 2 h / 80 °C
9.1: hydrogenchloride; water / 1,4-dioxane / 4 h / Heating / reflux
10.1: dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine / tetrahydrofuran; dichloromethane / 48 h / 20 °C
With
hydrogenchloride; dmap; potassium hydroxide; water; ammonium formate; phosphorus pentoxide; boron tribromide; potassium carbonate; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; N-ethyl-N,N-diisopropylamine; sodium iodide;
1,1'-bis-(diphenylphosphino)ferrocene; palladium diacetate; palladium 10% on activated carbon; nickel;
In
tetrahydrofuran; 1,4-dioxane; methanol; dichloromethane; o-xylene; water; dimethyl sulfoxide; N,N-dimethyl-formamide;
