1: 2-(4-fluoro-phenyl)-5-(4-methoxy-benzyloxymethyl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole With dihydrogen peroxide; acetic acid 48 h; 2: propylamine T=20°C;

1.1: NH4Cl / methanol / 3.5 h / 50 °C 2.1: ethyl acetate / 16 h / 20 °C 3.1: HBr; AcOH / aq. ethanol / 5.5 h / Heating 4.1: TBAF / tetrahydrofuran / 1 h / 0 - 20 °C 5.1: 99 percent / aq. NaOH; n-Bu4NHSO4 / 12 h / 20 °C 6.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 6.2: Bu3SnI 6.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 7.1: H2O2; AcOH / 48 h 7.2: 36 percent / 20 °C View Scheme

1.1: 99 percent / aq. NaOH; n-Bu4NHSO4 / 12 h / 20 °C 2.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 2.2: Bu3SnI 2.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 3.1: H2O2; AcOH / 48 h 3.2: 36 percent / 20 °C View Scheme

1.1: ethyl acetate / 16 h / 20 °C 2.1: HBr; AcOH / aq. ethanol / 5.5 h / Heating 3.1: TBAF / tetrahydrofuran / 1 h / 0 - 20 °C 4.1: 99 percent / aq. NaOH; n-Bu4NHSO4 / 12 h / 20 °C 5.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 5.2: Bu3SnI 5.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 6.1: H2O2; AcOH / 48 h 6.2: 36 percent / 20 °C View Scheme

1.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 1.2: Bu3SnI 1.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 2.1: H2O2; AcOH / 48 h 2.2: 36 percent / 20 °C View Scheme

1.1: TBAF / tetrahydrofuran / 1 h / 0 - 20 °C 2.1: 99 percent / aq. NaOH; n-Bu4NHSO4 / 12 h / 20 °C 3.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 3.2: Bu3SnI 3.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 4.1: H2O2; AcOH / 48 h 4.2: 36 percent / 20 °C View Scheme

1.1: 73 percent / CuBr2 / ethyl acetate / 5 h / Heating 2.1: ethyl acetate / 16 h / 20 °C 3.1: HBr; AcOH / aq. ethanol / 5.5 h / Heating 4.1: TBAF / tetrahydrofuran / 1 h / 0 - 20 °C 5.1: 99 percent / aq. NaOH; n-Bu4NHSO4 / 12 h / 20 °C 6.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 6.2: Bu3SnI 6.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 7.1: H2O2; AcOH / 48 h 7.2: 36 percent / 20 °C View Scheme

1.1: Lawesson's reagent / tetrahydrofuran / 2 h / 20 °C 2.1: CH2Cl2 / 5 h / 20 °C 3.1: NH4Cl / methanol / 3.5 h / 50 °C 4.1: ethyl acetate / 16 h / 20 °C 5.1: HBr; AcOH / aq. ethanol / 5.5 h / Heating 6.1: TBAF / tetrahydrofuran / 1 h / 0 - 20 °C 7.1: 99 percent / aq. NaOH; n-Bu4NHSO4 / 12 h / 20 °C 8.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 8.2: Bu3SnI 8.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 9.1: H2O2; AcOH / 48 h 9.2: 36 percent / 20 °C View Scheme

1.1: CH2Cl2 / 5 h / 20 °C 2.1: NH4Cl / methanol / 3.5 h / 50 °C 3.1: ethyl acetate / 16 h / 20 °C 4.1: HBr; AcOH / aq. ethanol / 5.5 h / Heating 5.1: TBAF / tetrahydrofuran / 1 h / 0 - 20 °C 6.1: 99 percent / aq. NaOH; n-Bu4NHSO4 / 12 h / 20 °C 7.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 7.2: Bu3SnI 7.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 8.1: H2O2; AcOH / 48 h 8.2: 36 percent / 20 °C View Scheme

1.1: 99 percent / aq. NaOH; n-Bu4NHSO4 / 12 h / 20 °C 2.1: n-BuLi / tetrahydrofuran / 0.5 h / -78 °C 2.2: Bu3SnI 2.3: 48 percent / Pd(PPh3)4 / dimethylformamide / 96 h / 80 °C 3.1: H2O2; AcOH / 48 h 3.2: 36 percent / 20 °C View Scheme