甲基1H-吡咯并[2,3-B]吡啶-5-甲酸酯合成路线 （共 11 条）
反应条件
palladium diacetate; 1,3-bis-(diphenylphosphino)propane in dimethyl sulfoxide T=100°C; P=15001.5 Torr; 48 h;
参考文献
WO2009/16460 A2, ;
Page/Page column 111 ;
WO 2009/016460 A2
反应条件
methanol; trans-di(μ-acetato)bis[o-(di-o-tolylphosphino)benzyl]dipalladium(II); triethylamine; 9,9-dimethyl-4,5-bis(diphenyl-phosphino)xanthene in tetrahydrofuran T=150°C; 0.166667 h; Microwave irradiation;
参考文献
ALLERGAN, INC.; CARLING, William R.; MARTOS, Jose L.; KANGASMETSA, Jussi J.; WANG, Jenny W.; WOODWARD, David F.
Patent: WO2013/96496 A2, 2013 ;
Location in patent: Page/Page column 78 ;
反应条件
sodium methylate in methanol T=65°C; 1 h;
参考文献
WO2005/28475 A2, ;
Page/Page column 141-142; 222 ;
WO 2005/028475 A2
反应条件
tetrabutyl ammonium fluoride in tetrahydrofuran T=25°C; 2 h; Reflux;
参考文献
US2011/144105 A1, ;
Page/Page column 11-12 ;
反应条件
1: N-ethyl-N,N-diisopropylamine; copper(l) iodide / tetrakis(triphenylphosphine) palladium(0) / N,N-dimethyl-formamide / 2 h / 0 - 25 °C 2: pyridine / dichloromethane / 12 h / 0 - 25 °C 3: tetrabutyl ammonium fluoride / tetrahydrofuran / 2 h / 25 °C / Reflux View Scheme
反应条件
1: iodine; silver trifluoroacetate / methanol / 72 h / 25 °C 2: N-ethyl-N,N-diisopropylamine; copper(l) iodide / tetrakis(triphenylphosphine) palladium(0) / N,N-dimethyl-formamide / 2 h / 0 - 25 °C 3: pyridine / dichloromethane / 12 h / 0 - 25 °C 4: tetrabutyl ammonium fluoride / tetrahydrofuran / 2 h / 25 °C / Reflux View Scheme
反应条件
1: pyridine / dichloromethane / 12 h / 0 - 25 °C 2: tetrabutyl ammonium fluoride / tetrahydrofuran / 2 h / 25 °C / Reflux View Scheme
反应条件
1: With potassium carbonate in N,N-dimethyl-formamide 2: With iodine in N,N-dimethyl-formamide T=20°C; 2 h;
参考文献
PFIZER INC.
Patent: US2012/270893 A1, 2012 ;
Location in patent: Page/Page column 25 ;
反应条件
lithium aluminium tetrahydride in tetrahydrofuran T=0°C; 12 h; Heating / reflux;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2005/28475 A2, 2005 ;
Location in patent: Page/Page column 142-143; 222 ;
WO 2005/028475 A2
反应条件
water; lithium hydroxide hydrate in tetrahydrofuran; methanol T=20°C; 3 h;
参考文献
Cheng, Huimin; Chang, Yu; Zhang, Lianwen; Luo, Jinfeng; Tu, Zhengchao; Lu, Xiaoyun; Zhang, Qingwen; Lu, Jibu; Ren, Xiaomei; Ding, Ke
Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2692 - 2703
