1: in N,N-dimethyl-formamide T=60°C; 2 h; 2: With ammonia in N,N-dimethyl-formamide T=0 - 5°C;

1.1: TFA / CH2Cl2 / 12 h / 20 °C 2.1: SOCl2 / 1,2-dichloro-ethane / 3 h / Heating 2.2: aq. NH3 / diethyl ether / 0.33 h / 0 °C View Scheme

1.1: n-BuLi / diethyl ether / -78 - 20 °C 2.1: TFA / CH2Cl2 / 12 h / 20 °C 3.1: SOCl2 / 1,2-dichloro-ethane / 3 h / Heating 3.2: aq. NH3 / diethyl ether / 0.33 h / 0 °C View Scheme

1: With thionyl chloride in 1,2-dichloro-ethane 3 h; Heating; 2: With ammonium hydroxide in diethyl ether T=0°C; 0.333333 h;

1.1: trichlorophosphate / 6 h / 160 - 165 °C / Sealed tube 2.1: N-ethyl-N,N-diisopropylamine; diphenyl phosphoryl azide / 6 h / Inert atmosphere; Reflux 3.1: N,N,N',N,-tetramethylethylenediamine; n-butyllithium / tetrahydrofuran / 2 h / -60 °C / Inert atmosphere 3.3: pH 2 4.1: 1,1'-carbonyldiimidazole / N,N-dimethyl-formamide / 2 h / 60 °C 4.2: 0 - 5 °C View Scheme

1.1: N-ethyl-N,N-diisopropylamine; diphenyl phosphoryl azide / 6 h / Inert atmosphere; Reflux 2.1: N,N,N',N,-tetramethylethylenediamine; n-butyllithium / tetrahydrofuran / 2 h / -60 °C / Inert atmosphere 2.3: pH 2 3.1: 1,1'-carbonyldiimidazole / N,N-dimethyl-formamide / 2 h / 60 °C 3.2: 0 - 5 °C View Scheme

1.1: NaHDMS / tetrahydrofuran / 3 h / 29 °C 2.1: n-BuLi / diethyl ether / -78 - 20 °C 3.1: TFA / CH2Cl2 / 12 h / 20 °C 4.1: SOCl2 / 1,2-dichloro-ethane / 3 h / Heating 4.2: aq. NH3 / diethyl ether / 0.33 h / 0 °C View Scheme

1: tert-butyl alcohol 2: n-butyllithium; N,N,N',N,-tetramethylethylenediamine 3: N,N-dimethyl-formamide; methanol; dichloromethane View Scheme

12 h; Heating;

1: 38 percent / 12 h / Heating 2: NEt3 / dioxane / 24 h / 80 °C View Scheme