2,4-二氯噻吩并[3,2-d]嘧啶合成路线 (共 13 条)
反应条件
N-ethyl-N,N-diisopropylamine; trichlorophosphate 2 h; Heating / reflux;
参考文献
Verheijen, Jeroen C.; Yu, Ker; Toral-Barza, Lourdes; Hollander, Irwin; Zask, Arie
Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 1 p. 375 - 379
参考文献
US2010/233164 A1, ;
US 20100233164 A1
反应条件
1.1: 2 h / 190 °C 1.2: Heating 2.1: trichlorophosphate / 10 h / Reflux View Scheme
参考文献
WO2011/130628 A1, ;
WO 2011/130628 A1
反应条件
1: T=200°C; 4 h; 2: With trichlorophosphate in acetonitrile 24 h; Reflux;
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 20, # 8 p. 2408 - 2411
反应条件
1.1: methanol / 1 h / 20 °C 2.1: lithium hexamethyldisilazane / tetrahydrofuran / 1 h / -78 °C 2.2: 2 h / -78 - 20 °C View Scheme
参考文献
Zhu, Wu Fu; Zhai, Xin; Li, Sai; Cao, Yun Yun; Gong, Ping; Liu, Ya Jing
Chinese Chemical Letters, 2012 , vol. 23, # 6 p. 703 - 706
反应条件
1.1: methanol / 1 h / 20 °C 2.1: lithium diisopropyl amide / hexane; tetrahydrofuran / 1 h / -78 °C 2.2: 11 h / -78 - 20 °C 3.1: titanium(IV) isopropylate; triethylamine / chloroform / Reflux 3.2: 12 h / 20 °C 4.1: sodium hydrogencarbonate / bis-triphenylphosphine-palladium(II) chloride / toluene; ethanol; water / 1 h / 120 °C / Inert atmosphere; Microwave irradiation View Scheme
参考文献
WO2011/130628 A1, ;
WO 2011/130628 A1
反应条件
hydrogen; sodium hydrogencarbonate; palladium 10 on activated carbon in ethanol; ethyl acetate 5 h;
参考文献
GATEKEEPER PHARMACEUTICAL, INC.; GRAY, Nathanael, S.; ZHOU, Wenjun
Patent: WO2011/79231 A1, 2011 ;
Location in patent: Page/Page column 82 ;
反应条件
in methanol T=20°C; 1 h;
参考文献
GENENTECH, INC.; PIRAMED LIMITED
Patent: WO2007/127183 A1, 2007 ;
Location in patent: Page/Page column 135-136 ;
WO 2007/127183 A1
反应条件
sodium hydroxide in tetrahydrofuran T=20°C; 4 h; Inert atmosphere;
参考文献
Deng, Jifeng; Peng, Li; Zhang, Guicheng; Lan, Xiaobing; Li, Chufang; Chen, Fuxin; Zhou, Yayao; Lin, Zuoxian; Chen, Ling; Dai, Renke; Xu, Hongjiang; Yang, Ling; Zhang, Xiquan; Hu, Wenhui
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 1 p. 71 - 76
反应条件
1: hydrogen; sodium hydrogencarbonate / palladium 10 on activated carbon / ethyl acetate; ethanol / 5 h 2: bromine; periodic acid / acetonitrile / 2 h / Reflux View Scheme
参考文献
GATEKEEPER PHARMACEUTICAL, INC.; GRAY, Nathanael, S.; ZHOU, Wenjun
Patent: WO2011/79231 A1, 2011 ;