1.1: 80 percent / aq. NaOH / tetrahydrofuran 2.1: diethyl ether 3.1: PPh3P; diisopropyl azodicarboxylate / tetrahydrofuran / 3 h 4.1: aq. NaOH / tetrahydrofuran / 1 h 5.1: Cs2CO3 / dimethylformamide / 0 °C 5.2: 5.3 g / dimethylformamide / 20 °C 6.1: morph-DAST / tetrahydrofuran / -78 - 20 °C 7.1: H2 / Pd/C / methanol 8.1: HCl / dioxane / 1.5 h View Scheme

1.1: Cs2CO3 / dimethylformamide / 0 °C 1.2: 5.3 g / dimethylformamide / 20 °C 2.1: morph-DAST / tetrahydrofuran / -78 - 20 °C 3.1: H2 / Pd/C / methanol 4.1: HCl / dioxane / 1.5 h View Scheme

1.1: diethyl ether 2.1: PPh3P; diisopropyl azodicarboxylate / tetrahydrofuran / 3 h 3.1: aq. NaOH / tetrahydrofuran / 1 h 4.1: Cs2CO3 / dimethylformamide / 0 °C 4.2: 5.3 g / dimethylformamide / 20 °C 5.1: morph-DAST / tetrahydrofuran / -78 - 20 °C 6.1: H2 / Pd/C / methanol 7.1: HCl / dioxane / 1.5 h View Scheme

1: morph-DAST / tetrahydrofuran / -78 - 20 °C 2: H2 / Pd/C / methanol 3: HCl / dioxane / 1.5 h View Scheme

1.1: PPh3P; diisopropyl azodicarboxylate / tetrahydrofuran / 3 h 2.1: aq. NaOH / tetrahydrofuran / 1 h 3.1: Cs2CO3 / dimethylformamide / 0 °C 3.2: 5.3 g / dimethylformamide / 20 °C 4.1: morph-DAST / tetrahydrofuran / -78 - 20 °C 5.1: H2 / Pd/C / methanol 6.1: HCl / dioxane / 1.5 h View Scheme

1: H2 / Pd/C / methanol 2: HCl / dioxane / 1.5 h View Scheme

1.1: aq. NaOH / tetrahydrofuran / 1 h 2.1: Cs2CO3 / dimethylformamide / 0 °C 2.2: 5.3 g / dimethylformamide / 20 °C 3.1: morph-DAST / tetrahydrofuran / -78 - 20 °C 4.1: H2 / Pd/C / methanol 5.1: HCl / dioxane / 1.5 h View Scheme

hydrogenchloride in 1,4-dioxane 1.5 h;