2-氰基-2-(5-硝基吡啶-2-基)乙酸叔丁酯合成路线 (共 6 条)
反应条件
1: toluene-4-sulfonic acid / toluene / 2 h / |Reflux 2: palladium 10 on activated carbon; hydrogen / tetrahydrofuran / 2 h / 20 °C / 7500.75 Torr 3: hydrogen; ammonium hydroxide / ethanol / 60 °C / 22502.3 Torr View Scheme
参考文献
ENSEMBLE THERAPEUTICS CORPORATION; ALEXANDER, Sethu L.; BRIGGS, Timothy F.; FAVALORO, Frank G., Jr.; HALE, Stephen P.; SEIGAL, Benjamin A.; SHORTSLEEVES, Kelley C.; SNEDEKER, Cheri; TAYLOR, Michael; TERRETT, Nicholas K.; YAN, Dingxue; NOWAK, Pawel, Wojciech; DENNY, Rajiah Aldrin; CHRUNYK, Boris Andrew; SAHASRABUDHE, Parag Vasant; WITHKA, Jane Marie
Patent: WO2014/66726 A2, 2014 ;
反应条件
hydrogenchloride in ethanol T=80°C; 4 h;
参考文献
Su, Weiguo; Zhang, Weihan; Yang, Haibin
Patent: US2013/190307 A1, 2013 ;
Location in patent: Paragraph 0146; 0148 ;
反应条件
potassium carbonate in tetrahydrofuran
T=70°C;
参考文献
ENSEMBLE THERAPEUTICS CORPORATION; ALEXANDER, Sethu L.; BRIGGS, Timothy F.; FAVALORO, Frank G., Jr.; HALE, Stephen P.; SEIGAL, Benjamin A.; SHORTSLEEVES, Kelley C.; SNEDEKER, Cheri; TAYLOR, Michael; TERRETT, Nicholas K.; YAN, Dingxue; NOWAK, Pawel, Wojciech; DENNY, Rajiah Aldrin; CHRUNYK, Boris Andrew; SAHASRABUDHE, Parag Vasant; WITHKA, Jane Marie
Patent: WO2014/66726 A2, 2014 ;
Location in patent: Paragraph 00190 ;
反应条件
1: 66 percent / POCl3; PCl5 / 3 h / 110 °C
2: K2CO3 / tetrahydrofuran / 24 h / Heating
View Scheme
参考文献
Kokars; Yanishevskii; Kampars
Chemistry of Heterocyclic Compounds, 2002 , vol. 38, # 7 p. 805 - 809
反应条件
1: 77 percent / aq. H2SO4; NaNO2 / 0 - 20 °C
2: 66 percent / POCl3; PCl5 / 3 h / 110 °C
3: K2CO3 / tetrahydrofuran / 24 h / Heating
View Scheme
参考文献
Kokars; Yanishevskii; Kampars
Chemistry of Heterocyclic Compounds, 2002 , vol. 38, # 7 p. 805 - 809
反应条件
1: toluene-4-sulfonic acid / toluene / 2 h / |Reflux
2: palladium 10 on activated carbon; hydrogen / tetrahydrofuran / 2 h / 20 °C / 7500.75 Torr
View Scheme
参考文献
ENSEMBLE THERAPEUTICS CORPORATION; ALEXANDER, Sethu L.; BRIGGS, Timothy F.; FAVALORO, Frank G., Jr.; HALE, Stephen P.; SEIGAL, Benjamin A.; SHORTSLEEVES, Kelley C.; SNEDEKER, Cheri; TAYLOR, Michael; TERRETT, Nicholas K.; YAN, Dingxue; NOWAK, Pawel, Wojciech; DENNY, Rajiah Aldrin; CHRUNYK, Boris Andrew; SAHASRABUDHE, Parag Vasant; WITHKA, Jane Marie
Patent: WO2014/66726 A2, 2014 ;