Technology Process of 5-[2-(2,6-difluoro-3,5-dimethoxyphenyl)ethyl]-N-[1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
There total 4 articles about 5-[2-(2,6-difluoro-3,5-dimethoxyphenyl)ethyl]-N-[1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
palladium diacetate; caesium carbonate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl;
In
1,4-dioxane;
at 100 ℃;
for 4h;
Inert atmosphere;
- Guidance literature:
-
Multi-step reaction with 5 steps
1: Selectfluor / acetonitrile / 12 h / 20 °C / Cooling with ice
2: tetrakis(triphenylphosphine) palladium(0); copper(l) iodide; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 1 h / 80 °C / Inert atmosphere
3: hydrogen; palladium 10% on activated carbon / methanol; tetrahydrofuran / 8 h / 60 °C / Inert atmosphere
4: copper dichloride; n-Amyl nitrite / acetonitrile / 4 h / 60 °C / Inert atmosphere
5: 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; caesium carbonate; palladium diacetate / 1,4-dioxane / 4 h / 100 °C / Inert atmosphere
With
copper(l) iodide; tetrakis(triphenylphosphine) palladium(0); n-Amyl nitrite; palladium 10% on activated carbon; hydrogen; palladium diacetate; caesium carbonate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; Selectfluor; N-ethyl-N,N-diisopropylamine; copper dichloride;
In
tetrahydrofuran; 1,4-dioxane; methanol; N,N-dimethyl-formamide; acetonitrile;
- Guidance literature:
-
Multi-step reaction with 4 steps
1: tetrakis(triphenylphosphine) palladium(0); copper(l) iodide; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 1 h / 80 °C / Inert atmosphere
2: hydrogen; palladium 10% on activated carbon / methanol; tetrahydrofuran / 8 h / 60 °C / Inert atmosphere
3: copper dichloride; n-Amyl nitrite / acetonitrile / 4 h / 60 °C / Inert atmosphere
4: 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; caesium carbonate; palladium diacetate / 1,4-dioxane / 4 h / 100 °C / Inert atmosphere
With
copper(l) iodide; tetrakis(triphenylphosphine) palladium(0); n-Amyl nitrite; palladium 10% on activated carbon; hydrogen; palladium diacetate; caesium carbonate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; N-ethyl-N,N-diisopropylamine; copper dichloride;
In
tetrahydrofuran; 1,4-dioxane; methanol; N,N-dimethyl-formamide; acetonitrile;
