Technology Process of 4-{3-[(4R,6S)-8-Chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]propanoyl}-2,6-piperazinedione
There total 11 articles about 4-{3-[(4R,6S)-8-Chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]propanoyl}-2,6-piperazinedione 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 72h;
- Guidance literature:
-
Multi-step reaction with 10 steps
1.1: trichlorophosphate / 0.17 h / 0 - 20 °C
1.2: 2 h / 50 °C / Heating / reflux
1.3: 0.5 h / Heating / reflux
2.1: toluene / 100 °C
3.1: sodium tetrahydroborate / methanol / 1 h / 20 °C
4.1: trifluoroacetic acid / dichloromethane / 20 °C
5.1: Resolution of racemate
6.1: lithium aluminium tetrahydride / tetrahydrofuran / 3 h / 0 °C
6.2: 3 h / 0 °C
7.1: triethylamine / dichloromethane / 3 h / 0 °C
8.1: dimethyl sulfoxide / 13 h / 50 °C
9.1: sodium hydroxide; water; isopropyl alcohol / 96 h / Heating / reflux
9.2: 0 °C
10.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 72 h / 20 °C
With
sodium hydroxide; sodium tetrahydroborate; lithium aluminium tetrahydride; water; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; isopropyl alcohol; trifluoroacetic acid; trichlorophosphate;
In
tetrahydrofuran; methanol; dichloromethane; dimethyl sulfoxide; toluene;
- Guidance literature:
-
Multi-step reaction with 9 steps
1.1: toluene / 100 °C
2.1: sodium tetrahydroborate / methanol / 1 h / 20 °C
3.1: trifluoroacetic acid / dichloromethane / 20 °C
4.1: Resolution of racemate
5.1: lithium aluminium tetrahydride / tetrahydrofuran / 3 h / 0 °C
5.2: 3 h / 0 °C
6.1: triethylamine / dichloromethane / 3 h / 0 °C
7.1: dimethyl sulfoxide / 13 h / 50 °C
8.1: sodium hydroxide; water; isopropyl alcohol / 96 h / Heating / reflux
8.2: 0 °C
9.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 72 h / 20 °C
With
sodium hydroxide; sodium tetrahydroborate; lithium aluminium tetrahydride; water; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; isopropyl alcohol; trifluoroacetic acid;
In
tetrahydrofuran; methanol; dichloromethane; dimethyl sulfoxide; toluene;