Technology Process of 3-[(4R,6S)-8-Chloro-6-(2,3-dimethoxyphenyl)-10-fluoro-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]propionic acid
There total 10 articles about 3-[(4R,6S)-8-Chloro-6-(2,3-dimethoxyphenyl)-10-fluoro-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]propionic acid which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
3-[(4R,6S)-8-Chloro-6-(2,3-dimethoxyphenyl)-10-fluoro-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]propanenitrile;
With
sodium hydroxide; water; isopropyl alcohol;
for 24h;
Heating / reflux;
With
hydrogenchloride; water;
at 0 ℃;
- Guidance literature:
-
Multi-step reaction with 10 steps
1.1: manganese(IV) oxide / dichloromethane / 14 h / 20 °C / Heating / reflux
2.1: trichlorophosphate / 0.25 h / 0 - 20 °C
2.2: 2.08 h / 0 - 50 °C
2.3: 0.5 h / 50 °C
3.1: toluene / 1 h / Heating / reflux
4.1: sodium tetrahydroborate / methanol / 1.5 h / 0 - 20 °C
4.2: 0 °C
5.1: trifluoroacetic acid / dichloromethane / 20 h / 0 - 20 °C
6.1: Resolution of racemate
7.1: lithium aluminium tetrahydride / tetrahydrofuran / 1 h / 0 °C
7.2: 0 °C
8.1: triethylamine / dichloromethane / 1 h / 0 °C
9.1: dimethyl sulfoxide / 13 h / 50 °C
10.1: sodium hydroxide; water; isopropyl alcohol / 24 h / Heating / reflux
10.2: 0 °C
With
manganese(IV) oxide; sodium hydroxide; sodium tetrahydroborate; lithium aluminium tetrahydride; water; triethylamine; isopropyl alcohol; trifluoroacetic acid; trichlorophosphate;
In
tetrahydrofuran; methanol; dichloromethane; dimethyl sulfoxide; toluene;
- Guidance literature:
-
Multi-step reaction with 8 steps
1.1: toluene / 1 h / Heating / reflux
2.1: sodium tetrahydroborate / methanol / 1.5 h / 0 - 20 °C
2.2: 0 °C
3.1: trifluoroacetic acid / dichloromethane / 20 h / 0 - 20 °C
4.1: Resolution of racemate
5.1: lithium aluminium tetrahydride / tetrahydrofuran / 1 h / 0 °C
5.2: 0 °C
6.1: triethylamine / dichloromethane / 1 h / 0 °C
7.1: dimethyl sulfoxide / 13 h / 50 °C
8.1: sodium hydroxide; water; isopropyl alcohol / 24 h / Heating / reflux
8.2: 0 °C
With
sodium hydroxide; sodium tetrahydroborate; lithium aluminium tetrahydride; water; triethylamine; isopropyl alcohol; trifluoroacetic acid;
In
tetrahydrofuran; methanol; dichloromethane; dimethyl sulfoxide; toluene;