2,4-二羟基吡咯[2,3-d]嘧啶合成路线 (共 8 条)
反应条件
sodium acetate in water T=70 - 80°C;
参考文献
Chen, Zecheng; Venkatesan, Aranapakam M.; Dehnhardt, Christoph M.; Ayral-Kaloustian, Semiramis; Brooijmans, Natasja; Mallon, Robert; Feldberg, Larry; Hollander, Irwin; Lucas, Judy; Yu, Ker; Kong, Fangming; Mansour, Tarek S.
Journal of Medicinal Chemistry, 2010 , vol. 53, # 8 p. 3169 - 3182
反应条件
1: urea With sodium ethanolate in ethanol T=5 - 10°C; 0.0833333 h; 2: 2-cyano-4,4-diethoxy-butyric acid ethyl ester in ethanol T=80°C; 3: With hydrogenchloride in water T=20°C;
参考文献
Xie, Hui; Zeng, Lili; Zeng, Shaogao; Lu, Xin; Zhang, Guicheng; Zhao, Xin; Cheng, Na; Tu, Zhengchao; Li, Zhiyuan; Xu, Hongjiang; Yang, Ling; Zhang, Xiquan; Huang, Min; Zhao, Junling; Hu, Wenhui
European Journal of Medicinal Chemistry, 2012 , vol. 52, p. 205 - 212
反应条件
hydrogenchloride; water T=20°C; 1.5 h;
参考文献
VERNALIS (R and D) LTD.
Patent: WO2007/104944 A1, 2007 ;
Location in patent: Page/Page column 38 ;
反应条件
hydrogenchloride; sodium acetate in water
参考文献
The Upjohn Company
Patent: US5502187 A1, 1996 ;
反应条件
1: 8 percent / phosphorus oxychloride, N,N-dimethylaniline / 2.5 h / Heating 2: 1.) NaH / 1.) acetonitrile, r.t., 30 min; 2.) 50 deg C, 2 h 3: 61 percent / ammonia / methanol / 12 h / 100 °C 4: 90 percent / K2CO3, hydrogen / 10percent Pd/C / aq. propan-1-ol / 2 h / 1520 Torr View Scheme
参考文献
Kazimierczuk, Zygmunt; Cottam, Howard B.; Revankar, Ganapathi R.; Robins, Roland K.
Journal of the American Chemical Society, 1984 , vol. 106, # 21 p. 6379 - 6382
反应条件
N-ethyl-N,N-diisopropylamine; trichlorophosphate in toluene T=70 - 80°C;
参考文献
Xie, Hui; Zeng, Lili; Zeng, Shaogao; Lu, Xin; Zhang, Guicheng; Zhao, Xin; Cheng, Na; Tu, Zhengchao; Li, Zhiyuan; Xu, Hongjiang; Yang, Ling; Zhang, Xiquan; Huang, Min; Zhao, Junling; Hu, Wenhui
European Journal of Medicinal Chemistry, 2012 , vol. 52, p. 205 - 212
反应条件
trichlorophosphate in water
参考文献
The Upjohn Company
Patent: US5502187 A1, 1996 ;
反应条件
1.1: N-ethyl-N,N-diisopropylamine; trichlorophosphate / toluene / 70 - 80 °C
2.1: sodium hydride / tetrahydrofuran / 0.5 h / 0 °C
2.2: 0 - 20 °C
View Scheme
参考文献
Xie, Hui; Zeng, Lili; Zeng, Shaogao; Lu, Xin; Zhang, Guicheng; Zhao, Xin; Cheng, Na; Tu, Zhengchao; Li, Zhiyuan; Xu, Hongjiang; Yang, Ling; Zhang, Xiquan; Huang, Min; Zhao, Junling; Hu, Wenhui
European Journal of Medicinal Chemistry, 2012 , vol. 52, p. 205 - 212