2,4-二氯-7H-吡咯并[2,3-d]嘧啶合成路线 （共 25 条）
反应条件
1: 2,4-dichloro-1H-pyrrololt;2,3-dgt;pyrimidine With sodium hydride in tetrahydrofuran T=0 - 20°C; 2: toluene-4-sulfonic acid in tetrahydrofuran T=20°C; 18 h;
参考文献
PALAU PHARMA, S.A.; SALAS SOLANA, Jorge; ALMANSA ROSALES, Carmen; SOLIVA SOLIVA, Robert; FONTES USTRELL, Montserrat; COMELLES ESPUGA, Josep
Patent: WO2010/34740 A1, 2010 ;
Location in patent: Page/Page column 67 ;
WO 2010/034740 A1
反应条件
1: tetrabutylammonium hydrogensulfate, 50percent aq. NaOH / CH2Cl2 2: 75 percent / conc. NH3 / dioxane / 24 h / 60 °C 3: 68 percent / CH3ONa / methanol / 3 h / Ambient temperature View Scheme
参考文献
Seela, Frank; Steker, Herbert; Driller, Hansjuergen; Bindig, Uwe
Liebigs Annalen der Chemie, 1987 , p. 15 - 19
反应条件
N-chloro-succinimide in N,N-dimethyl-formamide T=20°C; 48 h;
参考文献
GATEKEEPER PHARMACEUTICALS, INC.; GRAY, Nathanael, S.; ZHOU, Wenjun
Patent: WO2011/140338 A1, 2011 ;
Location in patent: Page/Page column 75 ;
反应条件
Selectfluorreg;; acetic acid in acetonitrile T=60°C; 5 h;
参考文献
Helvetica Chimica Acta, , vol. 91, # 6 p. 1083 - 1105
反应条件
potassium phosphate; palladium diacetate; 2-dicyclohexylphosphino-1,1'-biphenyl in 1,4-dioxane Suzuki coupling; 4 h; Inert atmosphereReflux;
参考文献
Dodonova, Jelena; Skardziute, Lina; Kazlauskas, Karolis; Jursenas, Saulius; Tumkevicius, Sigitas
Tetrahedron, 2012 , vol. 68, # 1 p. 329 - 339
反应条件
triethylamine in dichloromethane T=20°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: 2,4-dichloro-1H-pyrrololt;2,3-dgt;pyrimidine With sodium hydride in tetrahydrofuran T=0°C; 0.833333 h; 2: benzenesulfonyl chloride in tetrahydrofuran T=20°C; 1.5 h;
参考文献
VERNALIS (R and D) LTD.
Patent: WO2009/37467 A1, 2009 ;
Location in patent: Page/Page column 32-33; 15 ;
WO 2009/037467 A1
反应条件
ammonia in methanol T=100°C; 24 h;
参考文献
PORTOLA PHARMACEUTICALS, INC.
Patent: WO2009/131687 A2, 2009 ;
Location in patent: Page/Page column 148 ;
反应条件
in methanol
168 h; Heating;
参考文献
Seela, Frank; Driller, Hansjuergen; Liman, Ulrich
Liebigs Annalen der Chemie, 1985 , p. 312 - 320
反应条件
N-bromosuccinmide in dichloromethane
T=20°C;
参考文献
Seela, Frank; Xu, Kuiying
Helvetica Chimica Acta, 2008 , vol. 91, # 6 p. 1083 - 1105
