Multi-step reaction with 6 steps
1: caesium carbonate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2 / N,N-dimethyl-formamide; tetrahydrofuran / 2.5 h / 90 °C / Inert atmosphere
2: hydrogen / palladium 10% on activated carbon / methanol / 17 h / 20 °C
3: triethylamine / water; tetrahydrofuran / 0.17 h / 20 °C
4: diphenyl phosphoryl azide; 1,8-diazabicyclo[5.4.0]undec-7-ene / tetrahydrofuran / 25 h / 0 - 20 °C / Inert atmosphere
5: hydrogen / palladium 10% on activated carbon / methanol / 24 h / 20 °C
6: potassium hydroxide / tris-(dibenzylideneacetone)dipalladium(0); 5-(di-tert-butylphosphino)-1′, 3′, 5′-triphenyl-1′H-[1,4′]bipyrazole / water; tert-Amyl alcohol / 100 °C
With
diphenyl phosphoryl azide; hydrogen; caesium carbonate; 1,8-diazabicyclo[5.4.0]undec-7-ene; triethylamine; potassium hydroxide;
5-(di-tert-butylphosphino)-1′, 3′, 5′-triphenyl-1′H-[1,4′]bipyrazole; tris-(dibenzylideneacetone)dipalladium(0); dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; palladium 10% on activated carbon;
In
tetrahydrofuran; methanol; tert-Amyl alcohol; water; N,N-dimethyl-formamide;