2-氨基-5-氯-3-三甲基甲硅烷基乙酰基吡啶合成路线 （共 7 条）
反应条件
triethylamine; bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide in tetrahydrofuran T=20°C; 2 h;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED?
Patent: WO2005/95400 A1, 2005 ;
Location in patent: Page/Page column 345; 346 ;
WO 2005/095400 A1
反应条件
1.1: iodine; sulfuric acid; periodic acid / ethanol; water / 15 h / 80 °C 1.2: pH 9 2.1: triethylamine; copper(l) iodide / bis-triphenylphosphine-palladium(II) chloride / tetrahydrofuran / 1.67 h / 20 - 40 °C / Inert atmosphere View Scheme
反应条件
tetrabutyl ammonium fluoride in tetrahydrofuran T=20°C; 0.25 h;
参考文献
PFIZER PRODUCTS INC.
Patent: WO2008/4117 A1, 2008 ;
Location in patent: Page/Page column 103-104 ;
反应条件
1: potassium tert-butylate / 1-methyl-pyrrolidin-2-one / 4 h / 80 °C / Inert atmosphere 2: bromine; acetic acid / 3 h / 90 °C View Scheme
参考文献
MERCK SHARP and DOHME CORP.; CASH, Brandon; FISCHER, Christian; GARCIA, Yudith; JUNG, Joon; KATZ, Jason; KIM, June; RIVKIN, Alexey; SCHELL, Adam; SIU, Tony; WITTER, David; ZHOU, Hua
Patent: WO2011/137022 A1, 2011 ;
反应条件
potassium tert-butylate in 1-methyl-pyrrolidin-2-one T=80°C; 1 h; Inert atmosphere;
参考文献
CARNA BIOSCIENCES, INC.; SBI BIOTECH CO., LTD.; Irie, Takayuki; Sawa, Ayako; Sawa, Masaaki; Asami, Tokiko; Funakoshi, Yoko; Tanaka, Chika
Patent: US2014/18533 A1, 2014 ;
Location in patent: Paragraph 0078; 0079 ;
反应条件
1.1: potassium tert-butylate / 1-methyl-pyrrolidin-2-one / 4 h / 80 °C / Inert atmosphere
2.1: bromine; acetic acid / 3 h / 90 °C
3.1: sodium hydride / N,N-dimethyl-formamide; mineral oil / 0.83 h / 0 °C / Inert atmosphere
3.2: 1.5 h / 0 - 25 °C
View Scheme
参考文献
MERCK SHARP and DOHME CORP.; CASH, Brandon; FISCHER, Christian; GARCIA, Yudith; JUNG, Joon; KATZ, Jason; KIM, June; RIVKIN, Alexey; SCHELL, Adam; SIU, Tony; WITTER, David; ZHOU, Hua
Patent: WO2011/137022 A1, 2011 ;
反应条件
1.1: potassium tert-butylate / 1-methyl-pyrrolidin-2-one / 4 h / 80 °C / Inert atmosphere
2.1: bromine; acetic acid / 3 h / 90 °C
3.1: sodium hydride / N,N-dimethyl-formamide; mineral oil / 0.83 h / 0 °C / Inert atmosphere
3.2: 1.5 h / 0 - 25 °C
4.1: potassium acetate / palladium(II) dichloride bis[bis(diphenylphosphine)ferrocene] / ethylene glycol dimethyl ether / 6 h / 86 °C / Inert atmosphere
View Scheme
参考文献
MERCK SHARP and DOHME CORP.; CASH, Brandon; FISCHER, Christian; GARCIA, Yudith; JUNG, Joon; KATZ, Jason; KIM, June; RIVKIN, Alexey; SCHELL, Adam; SIU, Tony; WITTER, David; ZHOU, Hua
Patent: WO2011/137022 A1, 2011 ;
