3-[3-氟-4-[6-(2-甲基-2H-四唑-5-基)-3-吡啶基]苯基]-5-(羟基甲基)-2-恶唑烷酮合成路线 (共 4 条)
反应条件
lithium chloride; bis-triphenylphosphine-palladium(II) chloride in 1-methyl-pyrrolidin-2-one T=20 - 120°C; 4 h;
参考文献
Im, Weon Bin; Choi, Sun Ho; Park, Ju-Young; Choi, Sung Hak; Finn, John; Yoon, Sung-Hwa
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1027 - 1039
反应条件
1: benzyl (4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)carbamate With lithium hexamethyldisilazane in tetrahydrofuran T=20°C; 1.41667 h; Inert atmosphere; 2: (-)-(R)-glycidyl butyrate With N,N'-dimethyl-N,N'-propyleneurea in tetrahydrofuran T=20°C; 15 h; Inert atmospherecooling with ice;
参考文献
TRIUS THERAPEUTICS; COSTELLO, Carrie, A.; SIMSON, Jaqueline, A.; DUGUID, Robert, J.; PHILLIPSON, Douglas
Patent: WO2010/42887 A2, 2010 ;
Location in patent: Page/Page column 19-20 ;
反应条件
1: sodium cyanide / N,N-dimethyl-formamide / 7 h / 150 °C / Inert atmosphere 2: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 3 h / 110 °C / Inert atmosphere 3: sodium hydroxide / N,N-dimethyl-formamide / 0 - 20 °C / Inert atmosphere 4: bis-triphenylphosphine-palladium(II) chloride; lithium chloride / 1-methyl-pyrrolidin-2-one / 4 h / 120 °C / Inert atmosphere View Scheme
参考文献
European Journal of Medicinal Chemistry, , vol. 46, # 4 p. 1027 - 1039
反应条件
1: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 3 h / 110 °C / Inert atmosphere 2: sodium hydroxide / N,N-dimethyl-formamide / 0 - 20 °C / Inert atmosphere 3: bis-triphenylphosphine-palladium(II) chloride; lithium chloride / 1-methyl-pyrrolidin-2-one / 4 h / 120 °C / Inert atmosphere View Scheme
参考文献
European Journal of Medicinal Chemistry, , vol. 46, # 4 p. 1027 - 1039