1.1: 88 percent / I2; PPh3; imidazole 2.1: 98 percent / dioxane / 100 °C 3.1: 99 percent / toluene 4.1: NaOEt / ethanol / Heating 5.1: o-(NO2)C6H4SeCN; PBu3 / tetrahydrofuran 5.2: aq. H2O2 / tetrahydrofuran 6.1: 61 percent / MeLi / 0 °C 7.1: TBAF 8.1: PCC 9.1: 82 percent / NaH / tetrahydrofuran / 20 °C 10.1: 87 percent / AD-mix-α / 0 - 20 °C 11.1: MeC(OMe)3; PPTS / CH2Cl2 11.2: 88 percent / TMSCl; K2CO3 / methanol 12.1: DIBAL-H / toluene 13.1: DMF / 160 °C View Scheme

1.1: 98 percent / dioxane / 100 °C 2.1: 99 percent / toluene 3.1: NaOEt / ethanol / Heating 4.1: o-(NO2)C6H4SeCN; PBu3 / tetrahydrofuran 4.2: aq. H2O2 / tetrahydrofuran 5.1: 61 percent / MeLi / 0 °C 6.1: TBAF 7.1: PCC 8.1: 82 percent / NaH / tetrahydrofuran / 20 °C 9.1: 87 percent / AD-mix-α / 0 - 20 °C 10.1: MeC(OMe)3; PPTS / CH2Cl2 10.2: 88 percent / TMSCl; K2CO3 / methanol 11.1: DIBAL-H / toluene 12.1: DMF / 160 °C View Scheme

1.1: 99 percent / toluene 2.1: NaOEt / ethanol / Heating 3.1: o-(NO2)C6H4SeCN; PBu3 / tetrahydrofuran 3.2: aq. H2O2 / tetrahydrofuran 4.1: 61 percent / MeLi / 0 °C 5.1: TBAF 6.1: PCC 7.1: 82 percent / NaH / tetrahydrofuran / 20 °C 8.1: 87 percent / AD-mix-α / 0 - 20 °C 9.1: MeC(OMe)3; PPTS / CH2Cl2 9.2: 88 percent / TMSCl; K2CO3 / methanol 10.1: DIBAL-H / toluene 11.1: DMF / 160 °C View Scheme

1.1: NaOEt / ethanol / Heating 2.1: o-(NO2)C6H4SeCN; PBu3 / tetrahydrofuran 2.2: aq. H2O2 / tetrahydrofuran 3.1: 61 percent / MeLi / 0 °C 4.1: TBAF 5.1: PCC 6.1: 82 percent / NaH / tetrahydrofuran / 20 °C 7.1: 87 percent / AD-mix-α / 0 - 20 °C 8.1: MeC(OMe)3; PPTS / CH2Cl2 8.2: 88 percent / TMSCl; K2CO3 / methanol 9.1: DIBAL-H / toluene 10.1: DMF / 160 °C View Scheme

1.1: n-butyllithium; diisopropylamine / tetrahydrofuran; hexane / 0.5 h / -78 °C / Inert atmosphere 1.2: 1.5 h / -78 °C / Inert atmosphere 2.1: Pearlman's catalist; hydrogen / ethyl acetate / 6 h / 20 °C / Inert atmosphere 3.1: pyridine; 4-(N,N-dimethlyamino)pyridine / 0.75 h / 0 - 20 °C / Inert atmosphere 4.1: n-butyllithium; diisopropylamine / tetrahydrofuran; hexane / 0.5 h / -78 °C / Inert atmosphere 4.2: 12 h / -65 °C / Inert atmosphere 5.1: sodium tetrahydroborate / methanol / 2 h / 20 °C / Cooling with ice; Inert atmosphere 6.1: pyridine / 1.5 h / 0 - 20 °C / Inert atmosphere 7.1: potassium tert-butylate / tetrahydrofuran / 1.5 h / 0 °C / Inert atmosphere 8.1: methanesulfonamide; (DHQ)2-PHAL / water; tert-butyl alcohol / 72 h / 4 °C / Inert atmosphere 9.1: orthoacetic acid trimethyl ester; pyridinium p-toluenesulfonate / dichloromethane / 5 h / 20 °C / Inert atmosphere 9.2: 3 h / 20 °C / Inert atmosphere 9.3: 2 h / 20 °C / Inert atmosphere 10.1: diisobutylaluminium hydride / hexane; toluene / 0.33 h / -78 °C / Inert atmosphere 11.1: N,N-dimethyl-formamide / 4 h / Reflux; Inert atmosphere 12.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / tetrahydrofuran / 3 h / 0 °C / Inert atmosphere 13.1: hydrogenchloride; methanol / 5 h / 20 °C / Inert atmosphere 14.1: oxalyl dichloride; dimethyl sulfoxide / dichloromethane / -78 °C / Inert atmosphere 14.2: -78 - 0 °C / Inert atmosphere 15.1: potassium tert-butylate / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere 15.2: 0.5 h / 0 °C 16.1: methanol; potassium carbonate / 1.5 h / 20 °C / Inert atmosphere View Scheme

1.1: Pearlman's catalist; hydrogen / ethyl acetate / 6 h / 20 °C / Inert atmosphere 2.1: pyridine; 4-(N,N-dimethlyamino)pyridine / 0.75 h / 0 - 20 °C / Inert atmosphere 3.1: n-butyllithium; diisopropylamine / tetrahydrofuran; hexane / 0.5 h / -78 °C / Inert atmosphere 3.2: 12 h / -65 °C / Inert atmosphere 4.1: sodium tetrahydroborate / methanol / 2 h / 20 °C / Cooling with ice; Inert atmosphere 5.1: pyridine / 1.5 h / 0 - 20 °C / Inert atmosphere 6.1: potassium tert-butylate / tetrahydrofuran / 1.5 h / 0 °C / Inert atmosphere 7.1: methanesulfonamide; (DHQ)2-PHAL / water; tert-butyl alcohol / 72 h / 4 °C / Inert atmosphere 8.1: orthoacetic acid trimethyl ester; pyridinium p-toluenesulfonate / dichloromethane / 5 h / 20 °C / Inert atmosphere 8.2: 3 h / 20 °C / Inert atmosphere 8.3: 2 h / 20 °C / Inert atmosphere 9.1: diisobutylaluminium hydride / hexane; toluene / 0.33 h / -78 °C / Inert atmosphere 10.1: N,N-dimethyl-formamide / 4 h / Reflux; Inert atmosphere 11.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / tetrahydrofuran / 3 h / 0 °C / Inert atmosphere 12.1: hydrogenchloride; methanol / 5 h / 20 °C / Inert atmosphere 13.1: oxalyl dichloride; dimethyl sulfoxide / dichloromethane / -78 °C / Inert atmosphere 13.2: -78 - 0 °C / Inert atmosphere 14.1: potassium tert-butylate / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere 14.2: 0.5 h / 0 °C 15.1: methanol; potassium carbonate / 1.5 h / 20 °C / Inert atmosphere View Scheme

1.1: n-butyllithium; diisopropylamine / tetrahydrofuran; hexane / 0.5 h / -78 °C / Inert atmosphere 1.2: 12 h / -65 °C / Inert atmosphere 2.1: sodium tetrahydroborate / methanol / 2 h / 20 °C / Cooling with ice; Inert atmosphere 3.1: pyridine / 1.5 h / 0 - 20 °C / Inert atmosphere 4.1: potassium tert-butylate / tetrahydrofuran / 1.5 h / 0 °C / Inert atmosphere 5.1: methanesulfonamide; (DHQ)2-PHAL / water; tert-butyl alcohol / 72 h / 4 °C / Inert atmosphere 6.1: orthoacetic acid trimethyl ester; pyridinium p-toluenesulfonate / dichloromethane / 5 h / 20 °C / Inert atmosphere 6.2: 3 h / 20 °C / Inert atmosphere 6.3: 2 h / 20 °C / Inert atmosphere 7.1: diisobutylaluminium hydride / hexane; toluene / 0.33 h / -78 °C / Inert atmosphere 8.1: N,N-dimethyl-formamide / 4 h / Reflux; Inert atmosphere 9.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / tetrahydrofuran / 3 h / 0 °C / Inert atmosphere 10.1: hydrogenchloride; methanol / 5 h / 20 °C / Inert atmosphere 11.1: oxalyl dichloride; dimethyl sulfoxide / dichloromethane / -78 °C / Inert atmosphere 11.2: -78 - 0 °C / Inert atmosphere 12.1: potassium tert-butylate / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere 12.2: 0.5 h / 0 °C 13.1: methanol; potassium carbonate / 1.5 h / 20 °C / Inert atmosphere View Scheme

1.1: sodium tetrahydroborate / methanol / 2 h / 20 °C / Cooling with ice; Inert atmosphere 2.1: pyridine / 1.5 h / 0 - 20 °C / Inert atmosphere 3.1: potassium tert-butylate / tetrahydrofuran / 1.5 h / 0 °C / Inert atmosphere 4.1: methanesulfonamide; (DHQ)2-PHAL / water; tert-butyl alcohol / 72 h / 4 °C / Inert atmosphere 5.1: orthoacetic acid trimethyl ester; pyridinium p-toluenesulfonate / dichloromethane / 5 h / 20 °C / Inert atmosphere 5.2: 3 h / 20 °C / Inert atmosphere 5.3: 2 h / 20 °C / Inert atmosphere 6.1: diisobutylaluminium hydride / hexane; toluene / 0.33 h / -78 °C / Inert atmosphere 7.1: N,N-dimethyl-formamide / 4 h / Reflux; Inert atmosphere 8.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / tetrahydrofuran / 3 h / 0 °C / Inert atmosphere 9.1: hydrogenchloride; methanol / 5 h / 20 °C / Inert atmosphere 10.1: oxalyl dichloride; dimethyl sulfoxide / dichloromethane / -78 °C / Inert atmosphere 10.2: -78 - 0 °C / Inert atmosphere 11.1: potassium tert-butylate / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere 11.2: 0.5 h / 0 °C 12.1: methanol; potassium carbonate / 1.5 h / 20 °C / Inert atmosphere View Scheme

1.1: methanesulfonamide; (DHQ)2-PHAL / water; tert-butyl alcohol / 72 h / 4 °C / Inert atmosphere 2.1: orthoacetic acid trimethyl ester; pyridinium p-toluenesulfonate / dichloromethane / 5 h / 20 °C / Inert atmosphere 2.2: 3 h / 20 °C / Inert atmosphere 2.3: 2 h / 20 °C / Inert atmosphere 3.1: diisobutylaluminium hydride / hexane; toluene / 0.33 h / -78 °C / Inert atmosphere 4.1: N,N-dimethyl-formamide / 4 h / Reflux; Inert atmosphere 5.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / tetrahydrofuran / 3 h / 0 °C / Inert atmosphere 6.1: hydrogenchloride; methanol / 5 h / 20 °C / Inert atmosphere 7.1: oxalyl dichloride; dimethyl sulfoxide / dichloromethane / -78 °C / Inert atmosphere 7.2: -78 - 0 °C / Inert atmosphere 8.1: potassium tert-butylate / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere 8.2: 0.5 h / 0 °C 9.1: methanol; potassium carbonate / 1.5 h / 20 °C / Inert atmosphere View Scheme

1.1: orthoacetic acid trimethyl ester; pyridinium p-toluenesulfonate / dichloromethane / 5 h / 20 °C / Inert atmosphere 1.2: 3 h / 20 °C / Inert atmosphere 1.3: 2 h / 20 °C / Inert atmosphere 2.1: diisobutylaluminium hydride / hexane; toluene / 0.33 h / -78 °C / Inert atmosphere 3.1: N,N-dimethyl-formamide / 4 h / Reflux; Inert atmosphere 4.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / tetrahydrofuran / 3 h / 0 °C / Inert atmosphere 5.1: hydrogenchloride; methanol / 5 h / 20 °C / Inert atmosphere 6.1: oxalyl dichloride; dimethyl sulfoxide / dichloromethane / -78 °C / Inert atmosphere 6.2: -78 - 0 °C / Inert atmosphere 7.1: potassium tert-butylate / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere 7.2: 0.5 h / 0 °C 8.1: methanol; potassium carbonate / 1.5 h / 20 °C / Inert atmosphere View Scheme