1.1: potassium hydroxide / water / 4 h 1.2: 0.5 h / Cooling with ice-water bath 2.1: ethyl acetate / 1.25 h / 0 °C / Reflux 3.1: hydrogenchloride / dichloromethane; water / 0.08 h 4.1: oxalyl dichloride / N,N-dimethyl-formamide / dichloromethane / 15 - 25 °C 5.1: dichloromethane; water / 0 - 10 °C 6.1: borane-THF / tetrahydrofuran / 20 - 50 °C 6.2: 0.25 h / 0 - 5 °C 6.3: 2.5 h / 0 °C / Reflux 7.1: potassium carbonate; sodium iodide / 1-methyl-pyrrolidin-2-one / 20 - 60 °C / Inert atmosphere 7.2: 2 h / 20 °C 8.1: potassium carbonate / water / 0.08 h 8.2: Inert atmosphere View Scheme

1.1: potassium carbonate / 20 °C 2.1: potassium tert-butylate / dimethyl sulfoxide / 0.5 h / 20 °C 2.2: 20 °C View Scheme

chiralpak.(R).AD phase in ethanol; diethylamine; acetonitrile Resolution of racemate;

1.1: oxalyl dichloride / N,N-dimethyl-formamide / dichloromethane / 15 - 25 °C 2.1: dichloromethane; water / 0 - 10 °C 3.1: borane-THF / tetrahydrofuran / 20 - 50 °C 3.2: 0.25 h / 0 - 5 °C 3.3: 2.5 h / 0 °C / Reflux 4.1: potassium carbonate; sodium iodide / 1-methyl-pyrrolidin-2-one / 20 - 60 °C / Inert atmosphere 4.2: 2 h / 20 °C 5.1: potassium carbonate / water / 0.08 h 5.2: Inert atmosphere View Scheme

1.1: hydrogenchloride / dichloromethane; water / 0.33 h 2.1: oxalyl dichloride / N,N-dimethyl-formamide / dichloromethane / 15 - 25 °C 3.1: dichloromethane; water / 0 - 10 °C 4.1: borane-THF / tetrahydrofuran / 20 - 50 °C 4.2: 0.25 h / 0 - 5 °C 4.3: 2.5 h / 0 °C / Reflux 5.1: potassium carbonate; sodium iodide / 1-methyl-pyrrolidin-2-one / 20 - 60 °C / Inert atmosphere 5.2: 2 h / 20 °C 6.1: potassium carbonate / water / 0.08 h 6.2: Inert atmosphere View Scheme

1.1: hydrazine hydrate / ethanol / 4 h / Reflux 2.1: hydrogen / palladium 10 on activated carbon / ethanol; water / 12 h / 20 °C / 760.05 Torr 3.1: triethylamine / dichloromethane / 3 h / 0 - 20 °C 4.1: hydrogenchloride; water; acetic acid / 1 h / 25 °C 4.2: pH 9 / Cooling with ice View Scheme

1.1: hydrogen / palladium 10 on activated carbon / ethanol; water / 12 h / 20 °C / 760.05 Torr 2.1: triethylamine / dichloromethane / 3 h / 0 - 20 °C 3.1: hydrogenchloride; water; acetic acid / 1 h / 25 °C 3.2: pH 9 / Cooling with ice View Scheme

1.1: potassium carbonate; sodium iodide / 1-methyl-pyrrolidin-2-one / 20 - 60 °C / Inert atmosphere 1.2: 2 h / 20 °C 2.1: potassium carbonate / water / 0.08 h 2.2: Inert atmosphere View Scheme

1.1: borane-THF / tetrahydrofuran / 20 - 50 °C 1.2: 0.25 h / 0 - 5 °C 1.3: 2.5 h / 0 °C / Reflux 2.1: potassium carbonate; sodium iodide / 1-methyl-pyrrolidin-2-one / 20 - 60 °C / Inert atmosphere 2.2: 2 h / 20 °C 3.1: potassium carbonate / water / 0.08 h 3.2: Inert atmosphere View Scheme

1.1: dichloromethane; water / 0 - 10 °C 2.1: borane-THF / tetrahydrofuran / 20 - 50 °C 2.2: 0.25 h / 0 - 5 °C 2.3: 2.5 h / 0 °C / Reflux 3.1: potassium carbonate; sodium iodide / 1-methyl-pyrrolidin-2-one / 20 - 60 °C / Inert atmosphere 3.2: 2 h / 20 °C 4.1: potassium carbonate / water / 0.08 h 4.2: Inert atmosphere View Scheme