4-(4-碘苯基)四氢-1(2H)-吡嗪羧酸叔丁酯合成路线 （共 8 条）
反应条件
sodium hydroxide in water T=20°C;
参考文献
BRISTOL-MYERS SQUIBB PHARMA COMPANY
Patent: WO2008/83056 A2, 2008 ;
Location in patent: Page/Page column 60 ;
反应条件
water; iodine; sodium hydrogencarbonate in dichloromethane 0.5 h; Ambient temperature;
参考文献
La Clair, James J.
Angewandte Chemie - International Edition, 1998 , vol. 37, # 3 p. 325 - 329
反应条件
copper(l) iodide; sodium iodide; N-methyl-2-(methylamino)ethylamine in toluene T=110°C; 72 h;
参考文献
WO2007/97937 A1, ;
Page/Page column 193 ;
WO 2007/097937 A1
反应条件
triethylamine in dichloromethane T=20°C; 12 h; Inert atmosphere;
参考文献
Modi, Gyan; Antonio, Tamara; Reith, Maarten; Dutta, Aloke
Journal of Medicinal Chemistry, 2014 , vol. 57, # 4 p. 1557 - 1572
反应条件
1: 94 percent / DMAP, Et3N / CH2Cl2 / 1.5 h / Ambient temperature 2: 90 percent / I2, NaHCO3, H2O / CH2Cl2 / 0.5 h / Ambient temperature View Scheme
参考文献
Angewandte Chemie - International Edition, , vol. 37, # 3 p. 325 - 329
反应条件
1: 94 percent / DMAP, Et3N / CH2Cl2 / 1.5 h / Ambient temperature 2: 90 percent / I2, NaHCO3, H2O / CH2Cl2 / 0.5 h / Ambient temperature View Scheme
参考文献
Angewandte Chemie - International Edition, , vol. 37, # 3 p. 325 - 329
反应条件
1: tetrakis(triphenylphosphine) palladium(0); sodium carbonate / water; ethanol; ethylene glycol dimethyl ether / 1 h / 95 °C / |Inert atmosphere 2: trifluoroacetic acid / dichloromethane / 4 h / 20 °C / |Inert atmosphere View Scheme
参考文献
Modi, Gyan; Antonio, Tamara; Reith, Maarten; Dutta, Aloke
Journal of Medicinal Chemistry, 2014 , vol. 57, # 4 p. 1557 - 1572
反应条件
1: With n-butyllithium in tetrahydrofuran; hexane
T=-78°C; 0.5 h; Inert atmosphere;
2: With boric acid trimethyl ester in tetrahydrofuran; hexane
T=-78 - 20°C; Inert atmosphere;
3: With hydrogenchloride; water in tetrahydrofuran
T=20°C; pH=5 - 7;
参考文献
Ghosh, Balaram; Antonio, Tamara; Zhen, Juan; Kharkar, Prashant; Reith, Maarten E. A.; Dutta, Aloke K.
Journal of Medicinal Chemistry, 2010 , vol. 53, # 3 p. 1023 - 1037
