1: With methanesulfonic acid; water T=70°C; 10 h; Inert atmosphereLarge scale reaction; 2: With disodium hydrogenphosphate in water Inert atmosphereLarge scale reaction;

1.1: acetonitrile / 2 h / Reflux; Inert atmosphere; Large scale reaction 2.1: ethanol; acetyl chloride / 2 h / 45 °C / Inert atmosphere; Large scale reaction 3.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 4.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 4.2: Inert atmosphere; Large scale reaction View Scheme

1.1: 1,1'-bis-(diphenylphosphino)ferrocene; palladium diacetate; sodium carbonate / 105 °C / 15001.5 Torr / Autoclave 2.1: trifluoroacetic acid / ethanol / 20 h / 50 °C / Inert atmosphere 3.1: 4-methyl-morpholine / ethylene glycol dimethyl ether / 50 - 60 °C / Inert atmosphere; Large scale reaction 4.1: ethylene glycol dimethyl ether / 1.75 h / 65 °C / Inert atmosphere; Large scale reaction 5.1: ethanol; 1,8-diazabicyclo[5.4.0]undec-7-ene / 20 °C / Inert atmosphere 6.1: sulfuric acid / acetone / 0.83 h / 20 °C / Inert atmosphere; Large scale reaction 7.1: sodium hypochlorite; 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; tetraethylammonium bromide; sodium hydrogencarbonate / dichloromethane / 2 - 5 °C / Inert atmosphere 7.2: Inert atmosphere 8.1: dichloromethane / 20 °C / Inert atmosphere; Large scale reaction 9.1: dichloromethane / -15 - 0 °C / Inert atmosphere 10.1: sodium hydroxide / methanol; water / 5 - 40 °C / Inert atmosphere; Large scale reaction 10.2: pH 1 - 2 / Inert atmosphere; Large scale reaction 11.1: dichloromethane / 2 h / 20 °C / Inert atmosphere; Large scale reaction 12.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 13.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 13.2: Inert atmosphere; Large scale reaction View Scheme

1.1: trifluoroacetic acid / ethanol / 20 h / 50 °C / Inert atmosphere 2.1: 4-methyl-morpholine / ethylene glycol dimethyl ether / 50 - 60 °C / Inert atmosphere; Large scale reaction 3.1: ethylene glycol dimethyl ether / 1.75 h / 65 °C / Inert atmosphere; Large scale reaction 4.1: ethanol; 1,8-diazabicyclo[5.4.0]undec-7-ene / 20 °C / Inert atmosphere 5.1: sulfuric acid / acetone / 0.83 h / 20 °C / Inert atmosphere; Large scale reaction 6.1: sodium hypochlorite; 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; tetraethylammonium bromide; sodium hydrogencarbonate / dichloromethane / 2 - 5 °C / Inert atmosphere 6.2: Inert atmosphere 7.1: dichloromethane / 20 °C / Inert atmosphere; Large scale reaction 8.1: dichloromethane / -15 - 0 °C / Inert atmosphere 9.1: sodium hydroxide / methanol; water / 5 - 40 °C / Inert atmosphere; Large scale reaction 9.2: pH 1 - 2 / Inert atmosphere; Large scale reaction 10.1: dichloromethane / 2 h / 20 °C / Inert atmosphere; Large scale reaction 11.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 12.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 12.2: Inert atmosphere; Large scale reaction View Scheme

1.1: sodium hypochlorite; 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; tetraethylammonium bromide; sodium hydrogencarbonate / dichloromethane / 2 - 5 °C / Inert atmosphere 1.2: Inert atmosphere 2.1: dichloromethane / 20 °C / Inert atmosphere; Large scale reaction 3.1: dichloromethane / -15 - 0 °C / Inert atmosphere 4.1: sodium hydroxide / methanol; water / 5 - 40 °C / Inert atmosphere; Large scale reaction 4.2: pH 1 - 2 / Inert atmosphere; Large scale reaction 5.1: dichloromethane / 2 h / 20 °C / Inert atmosphere; Large scale reaction 6.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 7.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 7.2: Inert atmosphere; Large scale reaction View Scheme

1.1: dichloromethane / 20 °C / Inert atmosphere; Large scale reaction 2.1: dichloromethane / -15 - 0 °C / Inert atmosphere 3.1: sodium hydroxide / methanol; water / 5 - 40 °C / Inert atmosphere; Large scale reaction 3.2: pH 1 - 2 / Inert atmosphere; Large scale reaction 4.1: dichloromethane / 2 h / 20 °C / Inert atmosphere; Large scale reaction 5.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 6.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 6.2: Inert atmosphere; Large scale reaction View Scheme

1.1: hydrogenchloride / dichloromethane; water / Inert atmosphere; Large scale reaction 2.1: dichloromethane / 2 h / 20 °C / Inert atmosphere; Large scale reaction 3.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 4.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 4.2: Inert atmosphere; Large scale reaction View Scheme

1.1: hydrogenchloride / ethanol; water / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 5 - 10 °C / Inert atmosphere; Large scale reaction 3.1: acetonitrile / 2 h / Reflux; Inert atmosphere; Large scale reaction 4.1: ethanol; acetyl chloride / 2 h / 45 °C / Inert atmosphere; Large scale reaction 5.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 6.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 6.2: Inert atmosphere; Large scale reaction View Scheme

1.1: triethylamine / tetrahydrofuran / Inert atmosphere 2.1: 10 palladium on activated charcoal; hydrogen / ethanol 3.1: sodium carbonate / pentan-1-ol / Inert atmosphere 4.1: hydrogenchloride / ethanol; water / Inert atmosphere 5.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 5 - 10 °C / Inert atmosphere; Large scale reaction 6.1: acetonitrile / 2 h / Reflux; Inert atmosphere; Large scale reaction 7.1: ethanol; acetyl chloride / 2 h / 45 °C / Inert atmosphere; Large scale reaction 8.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 9.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 9.2: Inert atmosphere; Large scale reaction View Scheme

1.1: 10 palladium on activated charcoal; hydrogen / ethanol 2.1: sodium carbonate / pentan-1-ol / Inert atmosphere 3.1: hydrogenchloride / ethanol; water / Inert atmosphere 4.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 5 - 10 °C / Inert atmosphere; Large scale reaction 5.1: acetonitrile / 2 h / Reflux; Inert atmosphere; Large scale reaction 6.1: ethanol; acetyl chloride / 2 h / 45 °C / Inert atmosphere; Large scale reaction 7.1: triethylamine / dichloromethane / -10 °C / Inert atmosphere; Large scale reaction 8.1: methanesulfonic acid; water / 10 h / 70 °C / Inert atmosphere; Large scale reaction 8.2: Inert atmosphere; Large scale reaction View Scheme