4H-吡唑并[1,5-a]嘧啶-7-酮合成路线 (共 9 条)
反应条件
1: With sodium ethanolate in ethanol 1 h; Heating / reflux; 2: With acetic acid in ethanol; water T=0°C;
参考文献
Schering Corporation
Patent: US2007/82901 A1, 2007 ;
Location in patent: Page/Page column 21 ;
US 20070082901 A1
反应条件
1: ethyl acetate; formic acid ethyl ester With sodium in toluene T=20 - 40°C; 16 h; 2: 5-amino-1H-pyrazole in ethanol; toluene 4 h; Heating / reflux; 3: With hydrogenchloride in water
参考文献
EIRX THERAPEUTICS LIMITED
Patent: WO2007/17678 A1, 2007 ;
Location in patent: Page/Page column 43 ;
反应条件
1: ethyl acetate; formic acid ethyl ester With sodium in ethanol; toluene T=20°C; 16 h; 2: 5-amino-1H-pyrazole in ethanol; toluene T=80°C; 4 h; Further stages.;
参考文献
Gavrin, Lori K.; Lee, Arthur; Provencher, Brian A.; Massefski, Walter W.; Huhn, Stephen D.; Ciszewski, Gregory M.; Cole, Derek C.; McKew, John C.
Journal of Organic Chemistry, 2007 , vol. 72, # 3 p. 1043 - 1046
反应条件
dowtherm A T=250°C; 2 h;
参考文献
Gavrin, Lori K.; Lee, Arthur; Provencher, Brian A.; Massefski, Walter W.; Huhn, Stephen D.; Ciszewski, Gregory M.; Cole, Derek C.; McKew, John C.
Journal of Organic Chemistry, 2007 , vol. 72, # 3 p. 1043 - 1046
反应条件
1: 100 percent / aq. NaOH / ethanol / 3.5 h / 100 °C 2: 98 percent / Dowtherm A / 2 h / 250 °C View Scheme
参考文献
Gavrin, Lori K.; Lee, Arthur; Provencher, Brian A.; Massefski, Walter W.; Huhn, Stephen D.; Ciszewski, Gregory M.; Cole, Derek C.; McKew, John C.
Journal of Organic Chemistry, 2007 , vol. 72, # 3 p. 1043 - 1046
反应条件
in ethanol 5 h; Heating;
参考文献
Senga; Novinson; Wilson; Robins
Journal of Medicinal Chemistry, 1981 , vol. 24, # 5 p. 610 - 613
反应条件
in ethanol 6 h; Heating;
参考文献
Al-Saleh, Balkis; Makhseed, Saad; Hassaneen, Huwaida M. E.; Elnagdi, Mohamed Hilmy
Synthesis, 2006 , # 1 art. no. P06805SS, p. 59 - 62
反应条件
N-ethyl-N,N-diisopropylamine; trichlorophosphate T=90°C;
参考文献
ALMIRALL, S.A.; BERNAL ANCHUELA, Francisco Javier; CARRASCAL RIERA, Marta; CATURLA JAVALOYES, Juan Francisco; GRACIA FERRER, Jordi; MATASSA, Victor Giulio; TERRICABRAS BELART, Emma; TALTAVULL MOLL, Joan; ERRA SOLA, Montserrat
Patent: WO2012/146666 A1, 2012 ;
Location in patent: Page/Page column 160 ;
WO 2012/146666 A1
反应条件
1: 4,7-dihydropyrazololt;1,5-agt;pyrimidin-7-one With sodium hydride in N,N-dimethyl-formamide
T=0 - 20°C;
2: methyl iodide in N,N-dimethyl-formamide
T=20°C; 0.5 h; Further stages.;
参考文献
Gavrin, Lori K.; Lee, Arthur; Provencher, Brian A.; Massefski, Walter W.; Huhn, Stephen D.; Ciszewski, Gregory M.; Cole, Derek C.; McKew, John C.
Journal of Organic Chemistry, 2007 , vol. 72, # 3 p. 1043 - 1046