2,4-二氯吡咯并[3,2-d]嘧啶合成路线 （共 23 条）
反应条件
dichlorophenyl phosphine oxide; sodium hydroxide T=170 - 180°C; 3 h;
参考文献
Girgis, Nabih S.; Cottam, Howard B.; Larson, Steven B.; Robins, Roland K.
Journal of Heterocyclic Chemistry, 1987 , vol. 24, p. 821 - 827
反应条件
AlCl3, aluminium chloride in 1,2-dichloro-benzene T=160°C; 1.5 h;
参考文献
VALEANT RESEARCH and DEVELOPMENT
Patent: WO2006/122003 A2, 2006 ;
Location in patent: Page/Page column 33; 43-44 ;
WO 2006/122003 A2
反应条件
1: 81.2 percent / dimethylformamide / 0.5 h / 130 - 135 °C 2: 82.46 percent / Zn, acetic acid / 1 h / 70 - 80 °C 3: 60.6 percent / POCl3 / 6 h / Heating 4: 18 percent / POCl3, diethylaniline / 40 h / Heating View Scheme
参考文献
Pharmaceutical Chemistry Journal, , vol. 22, # 2 p. 135 - 141
Khimiko-Farmatsevticheskii Zhurnal, , vol. 22, # 2 p. 185 - 191
反应条件
1: 82.46 percent / Zn, acetic acid / 1 h / 70 - 80 °C 2: 60.6 percent / POCl3 / 6 h / Heating 3: 18 percent / POCl3, diethylaniline / 40 h / Heating View Scheme
参考文献
Pharmaceutical Chemistry Journal, , vol. 22, # 2 p. 135 - 141
Khimiko-Farmatsevticheskii Zhurnal, , vol. 22, # 2 p. 185 - 191
反应条件
N,N-diethylaniline; trichlorophosphate 48 h; Heating;
参考文献
Modnikova, G. A.; Titkova, R. M.; Glushkov, R. G.; Sokolova, A. S.; Silin, V. A.; Chernov, V. A.
Pharmaceutical Chemistry Journal, 1988 , vol. 22, # 2 p. 135 - 141
Khimiko-Farmatsevticheskii Zhurnal, 1988 , vol. 22, # 2 p. 185 - 191
反应条件
1: sulfuric acid; nitric acid / 20 °C 2: N,N-dimethyl-formamide / 80 - 140 °C 3: acetic acid; zinc / 80 °C 4: N-ethyl-N,N-diisopropylamine; trichlorophosphate / toluene / 70 - 80 °C View Scheme
参考文献
European Journal of Medicinal Chemistry, , vol. 52, p. 205 - 212
反应条件
N,N-diethylaniline; trichlorophosphate 40 h; Heating;
参考文献
Modnikova, G. A.; Titkova, R. M.; Glushkov, R. G.; Sokolova, A. S.; Silin, V. A.; Chernov, V. A.
Pharmaceutical Chemistry Journal, 1988 , vol. 22, # 2 p. 135 - 141
Khimiko-Farmatsevticheskii Zhurnal, 1988 , vol. 22, # 2 p. 185 - 191
反应条件
hydrogen; sodium hydrogencarbonate; palladium 10 on activated carbon in ethanol T=20°C; 3 h;
参考文献
CYTOPIA RESEARCH PTY LTD
Patent: WO2009/62258 A1, 2009 ;
Location in patent: Page/Page column 99 ;
WO 2009/062258 A1
反应条件
sodium hydride 1.) MeCN, RT, 30 min, 2.) a) 0-5 deg C, 15 min, b) RT, overnight; Yield given. Multistep reaction;
参考文献
JANSSEN RandD IRELAND; MC GOWAN, David Craig; LAST, Stefaan Julien; PIETERS, Serge Maria Aloysius; EMBRECHTS, Werner; JONCKERS, Tim Hugo Maria; RABOISSON, Pierre Jean-Marie Bernard
Patent: WO2014/56953 A1, 2014 ;
Location in patent: Page/Page column 8 ;
反应条件
1: 1.) NaH / 1.) MeCN, RT, 30 min, 2.) a) 0-5 deg C, 15 min, b) RT, overnight 2: 94 percent / NaOH / dioxane / 1 h / Heating View Scheme
参考文献
Girgis, Nabih S.; Michael, Maged A.; Smee, Donald F.; Alaghamandan, Hassan A.; Robins, Roland K.; Cottam, Howard B.
Journal of Medicinal Chemistry, 1990 , vol. 33, # 10 p. 2750 - 2755
