Technology Process of (R)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-[1,4]oxazepan-3-one
There total 8 articles about (R)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-[1,4]oxazepan-3-one which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
trimethylaluminum;
In
toluene;
at 23 ℃;
for 2h;
- Guidance literature:
-
Multi-step reaction with 6 steps
1: tetrahydrofuran; 2-methyltetrahydrofuran; (R)-N-((R)-2-(5-bromo-2,4-difluorophenyl)-3,3-difluoro-4-hydroxy-4-methylpentan-2-yl)-2-methylpropane-2-sulfinamide / 18 h / -78 - 23 °C
2: tetrakis(triphenylphosphine) palladium(0) / tetrahydrofuran / 8 h / 23 - 70 °C / Inert atmosphere
3: sodium periodate / ruthenium(III) trichloride hydrate / ethyl acetate; acetonitrile; water / 3 h / 23 °C
4: thionyl chloride / 18 h / 23 °C / Reflux
5: trifluorormethanesulfonic acid / dichloromethane / 0.5 h / 0 - 23 °C
6: trimethylaluminum / toluene / 2 h / 23 °C
With
sodium periodate; thionyl chloride; trifluorormethanesulfonic acid; trimethylaluminum;
tetrakis(triphenylphosphine) palladium(0); ruthenium(III) trichloride hydrate;
In
tetrahydrofuran; 2-methyltetrahydrofuran; dichloromethane; (R)-N-((R)-2-(5-bromo-2,4-difluorophenyl)-3,3-difluoro-4-hydroxy-4-methylpentan-2-yl)-2-methylpropane-2-sulfinamide; water; ethyl acetate; toluene; acetonitrile;
1: Grignard Reaction;
- Guidance literature:
-
Multi-step reaction with 4 steps
1: sodium periodate / ruthenium(III) trichloride hydrate / ethyl acetate; acetonitrile; water / 3 h / 23 °C
2: thionyl chloride / 18 h / 23 °C / Reflux
3: trifluorormethanesulfonic acid / dichloromethane / 0.5 h / 0 - 23 °C
4: trimethylaluminum / toluene / 2 h / 23 °C
With
sodium periodate; thionyl chloride; trifluorormethanesulfonic acid; trimethylaluminum;
ruthenium(III) trichloride hydrate;
In
dichloromethane; water; ethyl acetate; toluene; acetonitrile;