1.1: triethylamine; 4-(N,N-dimethlyamino)pyridine / 1 h / 0 °C 2.1: sodium hydride / dichloromethane; dimethyl sulfoxide; mineral oil / 8 h / 20 °C 3.1: boron trifluoride diethyl etherate / dichloromethane / 0.37 h / -15 °C 4.1: caesium carbonate / dimethyl sulfoxide / 0.25 h / 80 °C 4.2: 0.33 h / 80 °C 5.1: phosphoric acid / ethyl acetate; ethanol / 2 h / 50 °C View Scheme

1.1: sodium hydride / dichloromethane; dimethyl sulfoxide; mineral oil / 8 h / 20 °C 2.1: boron trifluoride diethyl etherate / dichloromethane / 0.37 h / -15 °C 3.1: caesium carbonate / dimethyl sulfoxide / 0.25 h / 80 °C 3.2: 0.33 h / 80 °C 4.1: phosphoric acid / ethyl acetate; ethanol / 2 h / 50 °C View Scheme

1.1: boron trifluoride diethyl etherate / dichloromethane / 0.37 h / -15 °C 2.1: caesium carbonate / dimethyl sulfoxide / 0.25 h / 80 °C 2.2: 0.33 h / 80 °C 3.1: phosphoric acid / ethyl acetate; ethanol / 2 h / 50 °C View Scheme

1: boron trifluoride diethyl etherate / 17 h / 0 - 20 °C 2: sulfuric acid / ethanol / 16 h / 78 °C 3: sodium carbonate / 0.5 h / 20 °C / pH 6.5 - 7 4: sodium azide / water; ethanol / 24 h / |Reflux 5: triphenylphosphine; acetic acid / water; tetrahydrofuran / 16 h / 45 °C 6: phosphoric acid / water; ethyl acetate; ethanol / 50 - 55 °C View Scheme

1: sulfuric acid / ethanol / 16 h / 78 °C 2: sodium carbonate / 0.5 h / 20 °C / pH 6.5 - 7 3: sodium azide / water; ethanol / 24 h / |Reflux 4: triphenylphosphine; acetic acid / water; tetrahydrofuran / 16 h / 45 °C 5: phosphoric acid / water; ethyl acetate; ethanol / 50 - 55 °C View Scheme

1.1: pyridine; sulfuryl dichloride / dichloromethane / -30 - -20 °C 2.1: perchloric acid / 18 h 3.1: dimethylsulfide borane complex; trimethylsilyl trifluoromethanesulfonate / dichloromethane / 1 h / -30 - -20 °C 3.2: 12 h / 20 °C 3.3: 2 h / 55 - 65 °C 4.1: sodium azide; ammonium chloride / water; ethanol / 8 h / 70 - 75 °C 4.2: 6 h / |Reflux 5.1: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 5 h / 8 - 85 °C 6.1: sodium hydrogencarbonate / water; dichloromethane / 1 h / 20 °C 7.1: hydrogen / ethanol / 18 h / 760.05 Torr 8.1: phosphoric acid / acetone; ethanol / |Reflux View Scheme

1.1: toluene-4-sulfonic acid / acetone / 2 h / |Reflux; |Large scale 2.1: ethanol / 2 h / 20 °C 2.2: 1 h / 0 - 10 °C 3.1: pyridine; sulfuryl dichloride / dichloromethane / -30 - -20 °C 4.1: perchloric acid / 18 h 5.1: dimethylsulfide borane complex; trimethylsilyl trifluoromethanesulfonate / dichloromethane / 1 h / -30 - -20 °C 5.2: 12 h / 20 °C 5.3: 2 h / 55 - 65 °C 6.1: sodium azide; ammonium chloride / water; ethanol / 8 h / 70 - 75 °C 6.2: 6 h / |Reflux 7.1: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 5 h / 8 - 85 °C 8.1: sodium hydrogencarbonate / water; dichloromethane / 1 h / 20 °C 9.1: hydrogen / ethanol / 18 h / 760.05 Torr 10.1: phosphoric acid / acetone; ethanol / |Reflux View Scheme

1.1: toluene-4-sulfonic acid / acetone / 2 h / |Reflux; |Large scale 2.1: ethanol / 2 h / 20 °C 2.2: 1 h / 0 - 10 °C 3.1: pyridine; sulfuryl dichloride / dichloromethane / -30 - -20 °C 4.1: perchloric acid / 18 h 5.1: dimethylsulfide borane complex; trimethylsilyl trifluoromethanesulfonate / dichloromethane / 1 h / -30 - -20 °C 5.2: 12 h / 20 °C 5.3: 2 h / 55 - 65 °C 6.1: sodium azide; ammonium chloride / water; ethanol / 8 h / 70 - 75 °C 6.2: 6 h / |Reflux 7.1: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 5 h / 8 - 85 °C 8.1: sodium hydrogencarbonate / water; dichloromethane / 1 h / 20 °C 9.1: hydrogen / ethanol / 18 h / 760.05 Torr 10.1: phosphoric acid / acetone; ethanol / |Reflux View Scheme

1.1: ethanol / 2 h / 20 °C 1.2: 1 h / 0 - 10 °C 2.1: pyridine; sulfuryl dichloride / dichloromethane / -30 - -20 °C 3.1: perchloric acid / 18 h 4.1: dimethylsulfide borane complex; trimethylsilyl trifluoromethanesulfonate / dichloromethane / 1 h / -30 - -20 °C 4.2: 12 h / 20 °C 4.3: 2 h / 55 - 65 °C 5.1: sodium azide; ammonium chloride / water; ethanol / 8 h / 70 - 75 °C 5.2: 6 h / |Reflux 6.1: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 5 h / 8 - 85 °C 7.1: sodium hydrogencarbonate / water; dichloromethane / 1 h / 20 °C 8.1: hydrogen / ethanol / 18 h / 760.05 Torr 9.1: phosphoric acid / acetone; ethanol / |Reflux View Scheme

1: boron trifluoride diethyl etherate / 17 h / 0 - 20 °C 2: sulfuric acid / ethanol / 16 h / 78 °C 3: sodium carbonate / 0.5 h / 20 °C / pH 6.5 - 7 4: sodium azide / water; ethanol / 24 h / |Reflux 5: 5 Pd/C; hydrogen / ethanol / 3 h / 24 °C View Scheme