Technology Process of (8R,9aS)-8-[(5-cyclopropylpyrazin-2-yl)oxy]-2-{[3-(trifluoromethyl)phenyl]acetyl}octahydro-5H-pyrrolo[1,2-a][1,4]diazepin-5-one
There total 10 articles about (8R,9aS)-8-[(5-cyclopropylpyrazin-2-yl)oxy]-2-{[3-(trifluoromethyl)phenyl]acetyl}octahydro-5H-pyrrolo[1,2-a][1,4]diazepin-5-one 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;
at 20 ℃;
for 16h;
- Guidance literature:
-
Multi-step reaction with 7 steps
1.1: isobutyl chloroformate; 4-methyl-morpholine / tetrahydrofuran / 0.5 h / -10 °C
1.2: 0.5 h / 0 °C
2.1: oxalyl dichloride; dimethyl sulfoxide / dichloromethane / 0.25 h / -78 °C
2.2: 0.5 h / -78 - 0 °C
3.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / 16 h / 10 - 25 °C
3.2: 0.5 h / 10 - 25 °C
3.3: 22 h / 5 - 25 °C
4.1: hydrogen; 20% palladium hydroxide-activated charcoal / ethanol / 15 h / 50 °C / 1551.49 Torr
5.1: potassium tert-butylate / tetrahydrofuran / 48 h / 20 °C
6.1: hydrogenchloride; methanol / 1,4-dioxane / 18 h / 20 °C
7.1: triethylamine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 16 h / 20 °C
With
4-methyl-morpholine; hydrogenchloride; methanol; oxalyl dichloride; 20% palladium hydroxide-activated charcoal; potassium tert-butylate; hydrogen; benzotriazol-1-ol; dimethyl sulfoxide; 1,8-diazabicyclo[5.4.0]undec-7-ene; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; isobutyl chloroformate;
In
tetrahydrofuran; 1,4-dioxane; ethanol; dichloromethane;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: oxalyl dichloride; dimethyl sulfoxide / dichloromethane / 0.25 h / -78 °C
1.2: 0.5 h / -78 - 0 °C
2.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / 16 h / 10 - 25 °C
2.2: 0.5 h / 10 - 25 °C
2.3: 22 h / 5 - 25 °C
3.1: hydrogen; 20% palladium hydroxide-activated charcoal / ethanol / 15 h / 50 °C / 1551.49 Torr
4.1: potassium tert-butylate / tetrahydrofuran / 48 h / 20 °C
5.1: hydrogenchloride; methanol / 1,4-dioxane / 18 h / 20 °C
6.1: triethylamine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 16 h / 20 °C
With
hydrogenchloride; methanol; oxalyl dichloride; 20% palladium hydroxide-activated charcoal; potassium tert-butylate; hydrogen; benzotriazol-1-ol; dimethyl sulfoxide; 1,8-diazabicyclo[5.4.0]undec-7-ene; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine;
In
tetrahydrofuran; 1,4-dioxane; ethanol; dichloromethane;
