1.1: 94 percent / diethyl ether 2.1: triphenylphosphine; diethyl azodicarboxylate / toluene; tetrahydrofuran 3.1: 5.18 g / NaOH / toluene; tetrahydrofuran / 1 h / 20 °C 4.1: Cs2CO3 / methanol; H2O 4.2: 88 percent / dimethylformamide / 0.5 h 5.1: 79.4 percent / morpholinosulphur trifluoride / tetrahydrofuran / 48 h / 20 °C 6.1: TFA / CH2Cl2 / 1 h / 20 °C 7.1: 2.22 g / N-methylmorpholine / CH2Cl2 / 6 h / 20 °C 8.1: 95.5 percent / acetic acid; zinc / 20 °C View Scheme

1.1: Cs2CO3 / methanol; H2O 1.2: 86.8 percent / dimethylformamide / 0.5 h 2.1: 94 percent / morpholinosulphur trifluoride / CH2Cl2 / 48 h / 20 °C 3.1: TFA / CH2Cl2 / 1 h / 20 °C 4.1: 5.41 g / N-methylmorpholine / CH2Cl2 / 6 h / 20 °C 5.1: 89.8 percent / acetic acid; zinc / 20 °C View Scheme