2,4-二氯-6-(4-氟苯基)嘧啶合成路线 （共 4 条）
反应条件
sodium carbonate; palladium diacetate; triphenylphosphine in tetrahydrofuran; water
T=60°C; Suzuki Coupling; 3 h; Inert atmosphere;
参考文献
Dr. Reddy's Laboratories Ltd.
Patent: US2010/144722 A1, 2010 ;
Location in patent: Page/Page column 26 ;
反应条件
1: 1-bromo-4-fluorobenzene With n-butyllithium in diethyl ether
T=-78°C; 0.75 h;
2: 2,4-Dichloro-pyrimidine in diethyl ether
T=-30 - 0°C; 1 h;
3: With sodium hydroxide; acetic acid; 2,3-dicyano-5,6-dichloro-p-benzoquinone
more than 3 stages;
参考文献
NEUROGEN CORPORATION
Patent: WO2005/7648 A2, 2005 ;
Location in patent: Page 95 ;
WO 2005/007648 A2
反应条件
palladium diacetate; sodium carbonate in tetrahydrofuran
T=60°C; Suzuki reaction; 3 h;
参考文献
Peng, Zhi-Hui; Journet, Michel; Humphrey, Guy
Organic Letters, 2006 , vol. 8, # 3 p. 395 - 398
反应条件
1: 1-bromo-4-fluorobenzene With n-butyllithium in diethyl ether
T=-78°C; 0.75 h;
2: 2,4-Dichloro-pyrimidine in diethyl ether
T=-30 - 0°C; 1 h;
3: With sodium hydroxide; water; acetic acid; 2,3-dicyano-5,6-dichloro-p-benzoquinone
Product distribution / selectivity; more than 3 stages;
参考文献
NEUROGEN CORPORATION
Patent: WO2006/26135 A2, 2006 ;
Location in patent: Page/Page column 65-66; 97 ;
WO 2006/026135 A2
