反应条件
1.1: bis(trimethylsilyl)trifluoroacetamide / dimethylformamide / 0.5 h / 20 °C
1.2: 82 percent / dimethylformamide / 18 h / 20 °C
2.1: N-methylmorpholine; isobutyl chloroformate / tetrahydrofuran / 0.33 h / -10 °C
2.2: tetrahydrofuran; diethyl ether / 0.75 h / 0 - 20 °C
3.1: aq. HBr; AcOH / tetrahydrofuran; diethyl ether / 0.75 h / 0 - 20 °C
4.1: KF / dimethylformamide / 4 h / 20 °C
5.1: 0.142 g / NaBH4 / methanol; tetrahydrofuran / 1 h / 0 °C
6.1: H2 / Pd/C / methanol / 2 h / 760 Torr
7.1: hydroxybenzotriazole hydrate; 1-ethyl-3-(3',3'-dimethyl-1'-aminopropyl)carbodiimide*HCl / CH2Cl2 / 0.17 h / 0 °C
7.2: N-methylmorpholine / CH2Cl2 / 16 h / 20 °C
8.1: 77 percent / iodobenzene diacetate; 2,2,6,6-tetramethyl-1-piperidinyloxy free radical / CH2Cl2 / 16 h / 20 °C
View Scheme
参考文献
Linton, Steven D.; Aja, Teresa; Armstrong, Robert A.; Bai, Xu; Chen, Long-Shiuh; Chen, Ning; Ching, Brett; Contreras, Patricia; Diaz, Jose-Luis; Fisher, Craig D.; Fritz, Lawrence C.; Gladstone, Patricia; Groessl, Todd; Gu, Xin; Herrmann, Julia; Hirakawa, Brad P.; Hoglen, Niel C.; Jahangiri, Kathy G.; Kalish, Vincent J.; Karanewsky, Donald S.; Kodandapani, Lalitha; Krebs, Joseph; McQuiston, Jeff; Meduna, Steven P.; Nalley, Kip; Robinson, Edward D.; Sayers, Robert O.; Sebring, Kristen; Spada, Alfred P.; Ternansky, Robert J.; Tomaselli, Kevin J.; Ullman, Brett R.; Valentino, Karen L.; Weeks, Suzanne; Winn, David; Wu, Joe C.; Yeo, Pauline; Zhang, Cheng-Zhi
Journal of Medicinal Chemistry, 2005 , vol. 48, # 22 p. 6779 - 6782
