反应条件
1.1: sodium hydride / N,N-dimethyl-formamide; mineral oil / 0 - 20 °C 1.2: 3 h / 0 - 20 °C 2.1: N-bromosuccinmide / dichloromethane / 20 °C 3.1: ammonium hydroxide / 48 h / 100 °C / |Autoclave 4.1: tris(dibenzylideneacetone)dipalladium(0) chloroform complex; tripotassium phosphate monohydrate; [(t-Bu)3PH]BF4 / 1,4-dioxane; water / 1.5 h / 85 °C / |Inert atmosphere 5.1: hydrogenchloride / water; ethanol / 5 h / 85 °C / |Inert atmosphere 6.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 4.5 h / 20 °C / |Cooling with ice View Scheme
参考文献
Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207