反应条件
1.1: di-tert-butylazodicarboxylate; triphenylphosphine / tetrahydrofuran; dichloromethane / -78 - 20 °C
1.2: 24 h / -78 - 20 °C
2.1: potassium hydrogencarbonate / water; ethyl acetate / 12 h / 20 °C
3.1: ammonium hydroxide / tetrahydrofuran; methanol / 20 °C
4.1: triethylamine; trifluoroacetic anhydride / dichloromethane / 2 h / 20 °C / Cooling with ice
5.1: sodium azide; pyridine hydrochloride / 1-methyl-pyrrolidin-2-one / 2 h / 130 °C
6.1: triethylamine / tetrahydrofuran / 2 h / Reflux
6.2: 3 h / 20 °C
View Scheme
参考文献
Oballa, Renata M.; Belair, Liette; Black, W. Cameron; Bleasby, Kelly; Chan, Chi Chung; Desroches, Carole; Du, Xiaobing; Gordon, Robert; Guay, Jocelyne; Guiral, Sebastien; Hafey, Michael J.; Hamelin, Emelie; Huang, Zheng; Kennedy, Brian; Lachance, Nicolas; Landry, France; Li, Chun Sing; Mancini, Joseph; Normandin, Denis; Pocai, Alessandro; Powell, David A.; Ramtohul, Yeeman K.; Skorey, Kathryn; Sorensen, Dan; Sturkenboom, Wayne; Styhler, Angela; Waddleton, Deena M.; Wang, Hao; Wong, Simon; Xu, Lijing; Zhang, Lei
Journal of Medicinal Chemistry, 2011 , vol. 54, # 14 p. 5082 - 5096