6-氯-4-(甲基氨基)烟酸乙酯合成路线 （共 6 条）
反应条件
1.1: lithium aluminium tetrahydride / tetrahydrofuran / -78 °C 1.2: 20 °C 2.1: manganese(IV) oxide / dichloromethane / 20 °C View Scheme
参考文献
WO2011/97526 A1, ;
WO 2011/097526 A1
反应条件
in water; acetonitrile
T=0 - 20°C; 3.5 h; regioselective reaction;
参考文献
Montoir, David; Tonnerre, Alain; Duflos, Muriel; Bazin, Marc-Antoine
European Journal of Organic Chemistry, 2014 , vol. 2014, # 7 p. 1487 - 1495
反应条件
N-ethyl-N,N-diisopropylamine in acetonitrile
T=70°C;
参考文献
BLUEPRINT MEDICINES; BIFULCO, Neil, Jr.; BROOIJMANS, Natasja; HODOUS, Brian, L.; KIM, Joseph, L.; MIDUTURU, Chandrasekhar, V.
Patent: WO2014/11900 A2, 2014 ;
Location in patent: Page/Page column 53; 54 ;
反应条件
1.1: acetic anhydride / 1.5 h / 120 °C
1.2: 0 °C / Cooling
1.3: pH < 5
2.1: trichlorophosphate / 3 h / 110 °C
3.1: acetonitrile; water / 3.5 h / 0 - 20 °C
View Scheme
参考文献
IRM LLC; NOVARTIS AG; TELLEW, John E.; PAN, Shifeng; WAN, Yongqin; XIE, Yongping; WANG, Xing; WANG, Xia; HUANG, Shenlin; LIU, Zuosheng; ZHANG, Qiong
Patent: WO2011/97526 A1, 2011 ;
WO 2011/097526 A1
反应条件
1: trichlorophosphate / 3 h / 110 °C
2: acetonitrile; water / 3.5 h / 0 - 20 °C
View Scheme
参考文献
IRM LLC; NOVARTIS AG; TELLEW, John E.; PAN, Shifeng; WAN, Yongqin; XIE, Yongping; WANG, Xing; WANG, Xia; HUANG, Shenlin; LIU, Zuosheng; ZHANG, Qiong
Patent: WO2011/97526 A1, 2011 ;
WO 2011/097526 A1
反应条件
lithium aluminium tetrahydride in tetrahydrofuran
T=0°C; 0.333333 h; Inert atmosphere;
参考文献
FLYNN, Daniel L.; KAUFMAN, Michael D.
Patent: WO2013/184119 A1, 2013 ;
Location in patent: Paragraph 0195 ;
