3-乙炔咪唑并[1,2-a]吡啶合成路线 （共 3 条）
反应条件
tetrabutyl ammonium fluoride in tetrahydrofuran; water
T=20°C; 2 h; Sonographic coupling;
参考文献
ARIAD PHARMACEUTICALS, INC.
Patent: WO2007/75869 A2, 2007 ;
Location in patent: Page/Page column 56-57 ;
反应条件
1: With bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide; N,N-dicyclohexylamine in acetonitrile
T=80°C; 3.25 h; Sealed tubeInert atmosphere;
2: With tetrabutyl ammonium fluoride in tetrahydrofuran
T=20°C; 2 h;
参考文献
ARIAD PHARMACEUTICALS, INC.; GOZGIT, Joseph, M.; RIVERA, Victor, M.; SHAKESPEARE, William, C.; ZHU, Xiaotian; DALGARNO, David, C.
Patent: WO2013/162727 A1, 2013 ;
Location in patent: Page/Page column 59 ;
反应条件
1: copper(l) iodide; triethylamine; bis-triphenylphosphine-palladium(II) chloride / acetonitrile / 20 h / |Reflux; |Inert atmosphere
2: potassium carbonate / methanol / 0.5 h / 20 °C / |Inert atmosphere
View Scheme
参考文献
Li, Yupeng; Shen, Mengjie; Zhang, Zhang; Luo, Jinfeng; Pan, Xiaofen; Lu, Xiaoyun; Long, Huoyou; Wen, Donghai; Zhang, Fengxiang; Leng, Fang; Li, Yingjun; Tu, Zhengchao; Ren, Xiaomei; Ding, Ke
Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 10033 - 10046
