Technology Process of 2-(2-{2-[(4R,6S)-8-Chloro-6-(2,3-dimethoxyphenyl)-10-fluoro-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-2H-1,2,3,4-tetrazol-5-yl)acetic acid
There total 12 articles about 2-(2-{2-[(4R,6S)-8-Chloro-6-(2,3-dimethoxyphenyl)-10-fluoro-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-2H-1,2,3,4-tetrazol-5-yl)acetic acid which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
potassium carbonate;
- Guidance literature:
-
Multi-step reaction with 11 steps
1.1: n-butyllithium / diethyl ether; hexane / 0.25 h / -78 - 0 °C
1.2: 1 h / -78 - 0 °C
2.1: manganese(IV) oxide / dichloromethane / 14 h / 20 °C / Heating / reflux
3.1: trichlorophosphate / 0.25 h / 0 - 20 °C
3.2: 2.08 h / 0 - 50 °C
3.3: 0.5 h / 50 °C
4.1: toluene / 1 h / Heating / reflux
5.1: sodium tetrahydroborate / methanol / 1.5 h / 0 - 20 °C
5.2: 0 °C
6.1: trifluoroacetic acid / dichloromethane / 20 h / 0 - 20 °C
7.1: Resolution of racemate
8.1: lithium aluminium tetrahydride / tetrahydrofuran / 1 h / 0 °C
8.2: 0 °C
9.1: triethylamine / dichloromethane / 1 h / 0 °C
10.1: potassium carbonate / tetra-(n-butyl)ammonium iodide / N,N-dimethyl-formamide / 2 h / 80 °C
11.1: potassium carbonate
With
manganese(IV) oxide; sodium tetrahydroborate; lithium aluminium tetrahydride; n-butyllithium; potassium carbonate; triethylamine; trifluoroacetic acid; trichlorophosphate;
tetra-(n-butyl)ammonium iodide;
In
tetrahydrofuran; methanol; diethyl ether; hexane; dichloromethane; N,N-dimethyl-formamide; 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: potassium carbonate / tetra-(n-butyl)ammonium iodide / N,N-dimethyl-formamide / 2 h / 80 °C
8.1: potassium carbonate
With
sodium tetrahydroborate; lithium aluminium tetrahydride; potassium carbonate; triethylamine; trifluoroacetic acid;
tetra-(n-butyl)ammonium iodide;
In
tetrahydrofuran; methanol; dichloromethane; N,N-dimethyl-formamide; toluene;