1: 96 percent / Et3N / various solvent(s) / 24 h / 50 °C 2: 78 percent / 4 mol dm-3 HCl / dioxane / 16 h / Ambient temperature View Scheme

toluene-4-sulfonic acid in 1,4-dioxane 6 h; Ambient temperature;

acetic acid T=50°C; 0.5 h;

1: 85 percent / Et3N / dimethylformamide / 3 h / Ambient temperature 2: 98 percent / NaH / dimethylformamide / 1.) 5 deg C to RT, 1 h; 2.) 1 h 3: 72 percent / N-methylmorpholine, tert-butyl hypochlorite / toluene / 1.) from -40- -50 deg C to RT, 3 h; 2.) 2 h 4: 51 percent / Mg / methanol / 4 h / 30 °C 5: 96 percent / p-TSA*H2O / dioxane / 6 h / Ambient temperature View Scheme

1: 98 percent / NaH / dimethylformamide / 1.) 5 deg C to RT, 1 h; 2.) 1 h 2: 81 percent / N-methylmorpholine, tert-butyl hypochlorite / toluene / 1.) from -40- -50 deg C to RT, 3 h; 2.) 2 h 3: 65 percent / Mg / methanol / 4 h / 30 °C 4: 83 percent / 80 percent aq. acetic acid / 0.5 h / 50 °C View Scheme

1: 84 percent / Et3N / dimethylformamide / 1.5 h / Ambient temperature 2: 98 percent / NaH / dimethylformamide / 1.) 5 deg C to RT, 1 h; 2.) 1 h 3: 81 percent / N-methylmorpholine, tert-butyl hypochlorite / toluene / 1.) from -40- -50 deg C to RT, 3 h; 2.) 2 h 4: 65 percent / Mg / methanol / 4 h / 30 °C 5: 83 percent / 80 percent aq. acetic acid / 0.5 h / 50 °C View Scheme

1: 98 percent / NaH / dimethylformamide / 1.) 5 deg C to RT, 1 h; 2.) 1 h 2: 81 percent / N-methylmorpholine, tert-butyl hypochlorite / toluene / 1.) from -40- -50 deg C to RT, 3 h; 2.) 2 h 3: 65 percent / Mg / methanol / 4 h / 30 °C 4: 83 percent / 80 percent aq. acetic acid / 0.5 h / 50 °C View Scheme

1: 65 percent / Mg / methanol / 4 h / 30 °C 2: 83 percent / 80 percent aq. acetic acid / 0.5 h / 50 °C View Scheme

1: 81 percent / N-methylmorpholine, tert-butyl hypochlorite / toluene / 1.) from -40- -50 deg C to RT, 3 h; 2.) 2 h 2: 65 percent / Mg / methanol / 4 h / 30 °C 3: 83 percent / 80 percent aq. acetic acid / 0.5 h / 50 °C View Scheme