5-氯-[1,2,4]三唑并[4,3-A]嘧啶-7-甲酸乙酯合成路线 （共 10 条）
反应条件
bromine; sodium acetate; acetic acid T=115°C;
参考文献
JANSSEN PHARMACEUTICA, N.V.
Patent: WO2006/130673 A1, 2006 ;
Location in patent: Page/Page column 74 ;
WO 2006/130673 A1
反应条件
sulfuric acid T=70°C; 20 h; Large scale;
参考文献
US2013/296302 A1, ;
Paragraph 0508 ;
反应条件
1: hydrazine hydrate / butan-1-ol / Reflux 2: sodium hydroxide; water; potassium permanganate / 80 - 90 °C 3: sulfuric acid / 6 h / Reflux; Inert atmosphere 4: sodium acetate; bromine; acetic acid / 120 °C / in a sealed tube View Scheme
反应条件
1.1: lithium diisopropyl amide / hexane; tetrahydrofuran; ethylbenzene / 3 h / -78 °C / Inert atmosphere 1.2: 2 h / -78 - -40 °C 1.3: -40 - -10 °C 2.1: chromium(VI) oxide / acetone / 3.25 h / -30 - 20 °C / Inert atmosphere 3.1: hydrazine hydrate / butan-1-ol / Reflux 4.1: sodium hydroxide; water; potassium permanganate / 80 - 90 °C 5.1: sulfuric acid / 6 h / Reflux; Inert atmosphere 6.1: sodium acetate; bromine; acetic acid / 120 °C / in a sealed tube View Scheme
反应条件
1: sodium hydroxide; water; potassium permanganate / 80 - 90 °C 2: sulfuric acid / 6 h / Reflux; Inert atmosphere 3: sodium acetate; bromine; acetic acid / 120 °C / in a sealed tube View Scheme
反应条件
1: chromium(VI) oxide / acetone / 3.25 h / -30 - 20 °C / Inert atmosphere 2: hydrazine hydrate / butan-1-ol / Reflux 3: sodium hydroxide; water; potassium permanganate / 80 - 90 °C 4: sulfuric acid / 6 h / Reflux; Inert atmosphere 5: sodium acetate; bromine; acetic acid / 120 °C / in a sealed tube View Scheme
反应条件
1: sulfuric acid / 6 h / Reflux; Inert atmosphere 2: sodium acetate; bromine; acetic acid / 120 °C / in a sealed tube View Scheme
反应条件
sodium hydroxide in methanol 4 h; Heating;
参考文献
JANSSEN PHARMACEUTICA, N.V.
Patent: WO2006/130673 A1, 2006 ;
Location in patent: Page/Page column 74 ;
WO 2006/130673 A1
反应条件
sodium hydride in tetrahydrofuran
参考文献
Lin, Ronghui; Connolly, Peter J.; Lu, Yanhua; Chiu, George; Li, Shengjian; Yu, Yang; Huang, Shenlin; Li, Xun; Emanuel, Stuart L.; Middleton, Steven A.; Gruninger, Robert H.; Adams, Mary; Fuentes-Pesquera, Angel R.; Greenberger, Lee M.
Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 15 p. 4297 - 4302
反应条件
1: 97 percent / NaH / tetrahydrofuran
2: 90 percent / aq. NaOH / methanol
View Scheme
参考文献
Lin, Ronghui; Connolly, Peter J.; Lu, Yanhua; Chiu, George; Li, Shengjian; Yu, Yang; Huang, Shenlin; Li, Xun; Emanuel, Stuart L.; Middleton, Steven A.; Gruninger, Robert H.; Adams, Mary; Fuentes-Pesquera, Angel R.; Greenberger, Lee M.
Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 15 p. 4297 - 4302
