Technology Process of R,S-2-[4-(1H-indol-3-yl)-trans-cyclohexylamino]-2-[1-(trans-3,5-difluorocinnamoyl)piperidin-4-yl]-acetamide
There total 12 articles about R,S-2-[4-(1H-indol-3-yl)-trans-cyclohexylamino]-2-[1-(trans-3,5-difluorocinnamoyl)piperidin-4-yl]-acetamide which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine;
In
dichloromethane; N,N-dimethyl-formamide;
at 20 ℃;
for 48h;
Inert atmosphere;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: potassium hydroxide / methanol / 4 h / 70 °C
2.1: hydrogen / palladium 10% on activated carbon / tetrahydrofuran / 4 h / 2327.23 Torr
3.1: hydrogenchloride / N,N-dimethyl-formamide; water / 24 h / 30 - 50 °C
4.1: titanium(IV) isopropylate / ethanol / 2 h / 20 °C / Inert atmosphere
4.2: 72 h / 20 °C / Inert atmosphere
5.1: hydrogenchloride / dichloromethane; 1,4-dioxane / 3 h / 50 °C
6.1: triethylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / dichloromethane; N,N-dimethyl-formamide / 48 h / 20 °C / Inert atmosphere
With
titanium(IV) isopropylate; hydrogenchloride; hydrogen; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; potassium hydroxide;
palladium 10% on activated carbon;
In
tetrahydrofuran; 1,4-dioxane; methanol; ethanol; dichloromethane; water; N,N-dimethyl-formamide;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: sodium azide / N,N-dimethyl-formamide / 24 h / 20 °C
2.1: hydrogen / palladium 10% on activated carbon / methanol / 24 h / 20 °C / Inert atmosphere
3.1: ammonia / methanol / 72 h / 100 °C
4.1: titanium(IV) isopropylate / ethanol / 2 h / 20 °C / Inert atmosphere
4.2: 72 h / 20 °C / Inert atmosphere
5.1: hydrogenchloride / dichloromethane; 1,4-dioxane / 3 h / 50 °C
6.1: triethylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / dichloromethane; N,N-dimethyl-formamide / 48 h / 20 °C / Inert atmosphere
With
titanium(IV) isopropylate; hydrogenchloride; sodium azide; ammonia; hydrogen; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine;
palladium 10% on activated carbon;
In
1,4-dioxane; methanol; ethanol; dichloromethane; N,N-dimethyl-formamide;