4-氯-6-乙基-5-氟嘧啶合成路线 （共 9 条）
反应条件
1: With triethylamine; trichlorophosphate in dichloromethane 5.5 h; Heating / reflux; 2: With hydrogenchloride; water in dichloromethane T=20°C;
参考文献
WO2009/20323 A2, ;
Page/Page column 7; 9 ;
反应条件
hydrogenchloride; triethylamine in dichloromethane
反应条件
1.1: sodium hydroxide / water / 0.5 h / 80 - 90 °C 1.2: pH 1 2.1: 5 palladium on charcoal; hydrogen / ethanol / 50 °C / 2585.81 Torr 3.1: triethylamine; trichlorophosphate / dichloromethane / 8 h / 40 °C / |Reflux View Scheme
参考文献
Organic Process Research and Development, , vol. 5, # 1 p. 28 - 36
反应条件
1: 1) MeONa, MeOH 2: POCl3 / Heating View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 6, # 16 p. 2031 - 2036
反应条件
N-ethyl-N,N-diisopropylamine in acetonitrile T=10 - 20°C; 2 h;
参考文献
HANMI PHARM. CO., LTD.
Patent: WO2009/20323 A2, 2009 ;
Location in patent: Page/Page column 9-10 ;
反应条件
N-bromosuccinmide; 2,2'-azo-bisisobutyronitrile in tetrachloromethane; dichloromethane T=75°C; 4 h; Heating / reflux;
参考文献
VIAMET PHARMACEUTICALS, INC.
Patent: WO2008/64311 A2, 2008 ;
Location in patent: Page/Page column 148 ;
反应条件
1: 4-chloro-6-ethyl-5-fluoropyrimidine With n-butyllithium; diisopropylamine in tetrahydrofuran; hexane; n-heptane T=-73 - 18°C; 2.25 h; 2: 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethan-1-one in tetrahydrofuran; hexane; n-heptane T=-74 - 55°C; 5 h;
参考文献
DR. REDDY'S LABORATORIES LTD.; DR. REDDY'S LABORATORIES, INC.
Patent: WO2006/65726 A2, 2006 ;
Location in patent: Page/Page column 17-18 ;
反应条件
lithium diisopropyl amide in tetrahydrofuran; n-heptane T=-70 - -65°C; pH=5 - 8; 3 - 4 h;
参考文献
MSN LABORATORIES LIMITED
Patent: WO2007/13096 A1, 2007 ;
Location in patent: Page/Page column 8 ;
反应条件
1: LDA / tetrahydrofuran 2: H2, AcONa / Pd/C / ethanol / 20 °C View Scheme
参考文献
GLENMARK GENERICS LIMITED
Patent: US2011/312977 A1, 2011 ;
