N-[(R)-(4-硝基苯氧基)苯氧基亚膦酰]-L-丙氨酸异丙酯合成路线 (共 2 条)
反应条件
1: β-D-2'-deoxy-2'-α-F-2'-β-C-methyluridine With 1,1-dimethylethylmagnesium chloride in tetrahydrofuran T=20°C; 0.5 h; 2: (S)-2-[(R)-(4-nitro-phenoxy)-phenoxy-phosphorylamino]propionic acid isopropyl ester; (S)-2-[(S)-(4-nitro-phenoxy)-phenoxy-phosphorylamino]propionic acid isopropyl ester in tetrahydrofuran T=20°C; 48 h;
参考文献
PHARMASSET, INC.; ROSS, Bruce, S.; SOFIA, Michael, Joseph; PAMULAPATI, Ganapati, Reddy; RACHAKONDA, Suguna; ZHANG, Hai-ren; CHUN, Byoung-kwon; WANG, Peiyuan
Patent: WO2010/135569 A1, 2010 ;
Location in patent: Page/Page column 47-48 ;
WO 2010/135569 A1
反应条件
Multi-step reaction with 3 steps 1: triethylamine / dichloromethane / 0.83 h / -78 °C2: dichloromethane / 1.25 h / 0 °C3: carbon dioxide / methanol; isopropyl alcohol / 75007.5 Torr / Supercritical conditions
参考文献
Ross, Bruce S.; Ganapati Reddy; Zhang, Hai-Ren; Rachakonda, Suguna; Sofia, Michael J. Journal of Organic Chemistry, 2011 , vol. 76, # 20 p. 8311 - 8319