反应条件
1.1: sulfuric acid / 16.5 h / 80 °C
2.1: dichloromethane / 2 h / 20 °C
3.1: dicyclohexyl(2′,6′-dimethoxybiphenyl-2-yl)phosphine; palladium diacetate; potassium phosphate / N,N-dimethyl-formamide; water / 21 h / 75 °C / |Inert atmosphere
4.1: pyridinium p-toluenesulfonate / methanol / 19 h / 50 °C
5.1: triethylamine; 4-(N,N-dimethlyamino)pyridine / dichloromethane / 0.33 h
5.2: 3 h / 20 °C
6.1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / N,N-dimethyl-formamide / 15 h / 90 °C
7.1: lithium aluminium tetrahydride / tetrahydrofuran; diethyl ether / 3.5 h / 0 - 40 °C
8.1: thionyl chloride / dichloromethane; N,N-dimethyl-formamide / 1 h / 0 - 20 °C
9.1: caesium carbonate / N,N-dimethyl-formamide / 20 °C
10.1: lithium hydroxide hydrate / tetrahydrofuran; methanol / 20 °C
View Scheme
参考文献
Brown, Sean P.; Dransfield, Paul J.; Vimolratana, Marc; Jiao, Xianyun; Zhu, Liusheng; Pattaropong, Vatee; Sun, Ying; Liu, Jinqian; Luo, Jian; Zhang, Jane; Wong, Simon; Zhuang, Run; Guo, Qi; Li, Frank; Medina, Julio C.; Swaminath, Gayathri; Lin, Daniel C.-H.; Houze, Jonathan B.
ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 9 p. 726 - 730
