5-(溴甲基)-4-(4-氟苯基)-6-异丙基-2-[甲基(甲磺酰)氨基]嘧啶合成路线 （共 15 条）
反应条件
hydrogen bromide in water T=80°C; 15 h;
参考文献
YUHAN CORPORATION; JU, Hyun; JOUNG, Sang-Sun; YI, Hyun-Jik; KHOO, Ja-Heouk; LIM, Jong-Chul; KIM, Jae-Gyu
Patent: WO2012/2741 A2, 2012 ;
Location in patent: Page/Page column 19 ;
WO 2012/002741 A2
反应条件
phosphorus tribromide in toluene; acetonitrile T=10 - 20°C; 1 h; Inert atmosphere;
参考文献
Kaneka Corporation
Patent: EP2351762 A1, 2011 ;
Location in patent: Page/Page column 9 ;
反应条件
N-bromosuccinmide in acetonitrile 0.5 h; UV-irradiationInert atmosphereSealed flow reactor; Product distribution / selectivity;
参考文献
LEK PHARMACEUTICALS D.D.; CASAR, Zdenko; STERK, Damjan; JUKIC, Marko
Patent: WO2012/13325 A1, 2012 ;
Location in patent: Page/Page column 57-58 ;
反应条件
1: potassium carbonate / acetone / 24 h / 20 °C 2: caesium carbonate / 2-methyl tetrahydrofuran / 10 h / 40 °C 3: triethylamine / dichloromethane / 8 h / -5 °C / Inert atmosphere 4: N-bromosuccinmide / acetonitrile / 0.5 h / UV-irradiation; Inert atmosphere; Sealed flow reactor View Scheme
反应条件
1: caesium carbonate / 2-methyl tetrahydrofuran / 10 h / 40 °C 2: triethylamine / dichloromethane / 8 h / -5 °C / Inert atmosphere 3: N-bromosuccinmide / acetonitrile / 0.5 h / UV-irradiation; Inert atmosphere; Sealed flow reactor View Scheme
反应条件
1: triethylamine / dichloromethane / 8 h / -5 °C / Inert atmosphere 2: N-bromosuccinmide / acetonitrile / 0.5 h / UV-irradiation; Inert atmosphere; Sealed flow reactor View Scheme
反应条件
1: diisobutylaluminium hydride / toluene / -78 - 0 °C / Inert atmosphere 2: triethylamine; methanesulfonyl chloride / dichloromethane / 5 h / 0 - 25 °C 3: hydrogen bromide / water / 15 h / 80 °C View Scheme
参考文献
WO2012/2741 A2, ;
WO 2012/002741 A2
反应条件
1: toluene / 3 h / 0 - 20 °C 2: potassium carbonate / N,N-dimethyl-formamide / 6 h / 70 - 75 °C 3: sulfuric acid / acetonitrile / 3 h / 50 - 60 °C View Scheme
参考文献
YUHAN CORPORATION; JU, Hyun; JOUNG, Sang-Sun; YI, Hyun-Jik; KHOO, Ja-Heouk; LIM, Jong-Chul; KIM, Jae-Gyu
Patent: WO2012/2741 A2, 2012 ;
WO 2012/002741 A2
反应条件
1.1: sodium hydroxide / water; acetone 2.1: tetrabutylammomium bromide; dihydrogen peroxide / dichloromethane; water / 10 - 20 °C 2.2: 0.5 h / 20 °C 3.1: dichloromethane; water / 2 h / 20 °C 3.2: 0.5 h / Reflux 4.1: sodium t-butanolate / tetrahydrofuran / -20 - -15 °C View Scheme
反应条件
in toluene T=60°C; 3 h;
参考文献
WO2004/103977 A2, ;
Page 24-25 ;
