反应条件
1.1: sodium hexamethyldisilazane / tetrahydrofuran / -78 °C 1.2: -78 - 20 °C 2.1: caesium carbonate; 9,9-dimethyl-4,5-bis(diphenyl-phosphino)xanthene / tris-(dibenzylideneacetone)dipalladium(0) / 1,4-dioxane / 90 °C 3.1: hydrogenchloride / water; tetrahydrofuran / 0.03 h 4.1: N-iodo-succinimide / acetonitrile / 0.83 h / 0 °C 5.1: tris-(dibenzylideneacetone)dipalladium(0) / isobutyramide / 6 h / 60 °C / Inert atmosphere 6.1: caesium carbonate / N,N-dimethyl-formamide / 1 h / 60 °C 7.1: sodium hydroxide; water / ethanol / 3 h / 60 °C 8.1: 4-(N,N-dimethlyamino)pyridine; 4-methyl-morpholine; HATU / acetonitrile / 5.75 h / 20 - 50 °C 9.1: trifluoroacetic acid / dichloromethane / 0.75 h / 20 °C 10.1: sodium hydride / N,N-dimethyl-formamide / 1 h / 20 °C 10.2: 72 h 11.1: acetic acid / 4 h / 35 °C 11.2: 6 h / 60 °C View Scheme
参考文献
BRISTOL-MYERS SQUIBB COMPANY; PURANDARE, Ashok V.; GREBINSKI, James W.; HART, Amy; INGHRIM, Jennifer; SCHROEDER, Gretchen; WAN, Honghe
Patent: WO2011/28864 A1, 2011 ;
WO 2011/028864 A1