1: 5-methyl-2-(pyrimidin-2-yl)benzoic acid With 2,6-dimethylpyridine; pivaloyl chloride in N,N-dimethyl-formamide T=5 - 10°C; 0.5 h; Inert atmosphere; 2: C12H17FN2O*(x)ClH With 2,6-dimethylpyridine; 1-propanephosphonic acid cyclic anhydride in N,N-dimethyl-formamide T=10 - 25°C;

1-propanephosphonic acid cyclic anhydride; N-ethyl-N,N-diisopropylamine in dichloromethane T=12 - 44°C;

1,3-propylenephosphoric acid; N-ethyl-N,N-diisopropylamine in dichloromethane T=12 - 46.7°C; 60.5 h;

1: tetrahydrofuran / 1.75 h / 20 °C / |Large scale 2: triethylamine / dichloromethane / 3 h / |Large scale 3: pyridine / 18 h / 10 - 20 °C 4: caesium carbonate / 1-methyl-pyrrolidin-2-one / 16 h / 60 °C / |Large scale 5: trifluoroacetic acid / dichloromethane / 4.17 h / -2 - 20 °C / |Large scale 6: N-ethyl-N,N-diisopropylamine; 1-propanephosphonic acid cyclic anhydride / dichloromethane / 18 h / 12 - 44 °C / |Large scale View Scheme

1: triethylamine / dichloromethane / 3 h / |Large scale 2: pyridine / 18 h / 10 - 20 °C 3: caesium carbonate / 1-methyl-pyrrolidin-2-one / 16 h / 60 °C / |Large scale 4: trifluoroacetic acid / dichloromethane / 4.17 h / -2 - 20 °C / |Large scale 5: N-ethyl-N,N-diisopropylamine; 1-propanephosphonic acid cyclic anhydride / dichloromethane / 18 h / 12 - 44 °C / |Large scale View Scheme

1: caesium carbonate / 1-methyl-pyrrolidin-2-one / 16 h / 60 °C / |Large scale 2: trifluoroacetic acid / dichloromethane / 4.17 h / -2 - 20 °C / |Large scale 3: N-ethyl-N,N-diisopropylamine; 1-propanephosphonic acid cyclic anhydride / dichloromethane / 18 h / 12 - 44 °C / |Large scale View Scheme

1: pyridine / 18 h / 10 - 20 °C 2: caesium carbonate / 1-methyl-pyrrolidin-2-one / 16 h / 60 °C / |Large scale 3: trifluoroacetic acid / dichloromethane / 4.17 h / -2 - 20 °C / |Large scale 4: N-ethyl-N,N-diisopropylamine; 1-propanephosphonic acid cyclic anhydride / dichloromethane / 18 h / 12 - 44 °C / |Large scale View Scheme

1.1: isopropylmagnesium chloride / tetrahydrofuran / 3.5 h / -15 - -12 °C / Inert atmosphere 1.2: 0.5 h / -12 - 2 °C 1.3: 17 h / 55 °C 2.1: hydrogenchloride; water / acetonitrile / 50 h / 10 - 22 °C 3.1: 2,6-dimethylpyridine; pivaloyl chloride / N,N-dimethyl-formamide / 0.5 h / 5 - 10 °C / Inert atmosphere 3.2: 10 - 25 °C View Scheme

1: trifluoroacetic acid / dichloromethane / 4.17 h / -2 - 20 °C / |Large scale 2: N-ethyl-N,N-diisopropylamine; 1-propanephosphonic acid cyclic anhydride / dichloromethane / 18 h / 12 - 44 °C / |Large scale View Scheme

1: sulfuric acid / methanol / 18 h / 65 °C / |Large scale 2: triethylamine; palladium diacetate; tris-(o-tolyl)phosphine / 2-methyl tetrahydrofuran / 1 h / 60 - 77 °C / |Inert atmosphere; |Large scale 3: sodium carbonate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / water; 2-methyl tetrahydrofuran / 16 h / 74 °C / |Inert atmosphere; |Large scale 4: sodium hydroxide / water; 2-methyl tetrahydrofuran / 1.5 h / 72 °C / |Large scale 5: N-ethyl-N,N-diisopropylamine; 1-propanephosphonic acid cyclic anhydride / dichloromethane / 18 h / 12 - 44 °C / |Large scale View Scheme