5-((Z)-(5-氟-2-氧代吲哚烷-3-亚基)甲基)-2,4-二甲基-1H-吡咯-3-羧酸合成路线 （共 13 条）
反应条件
1: 5-Fluoro-1,3-dihydro-2H-indol-2-one With ammonium sulfate; 1,1,1,3,3,3-hexamethyl-disilazane 5 h; Reflux; 2: 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid With trimethylsilyl trifluoromethanesulfonate
参考文献
SCINOPHARM TAIWAN, LTD.; Henscheke, Julian P.; Chen, Yung-Fa
Patent: US2013/190512 A1, 2013 ;
Location in patent: Paragraph 0088 ;
反应条件
hydrogenchloride; acetic acid in ethanol; water; acetone
参考文献
Tang, Peng Cho; Miller, Todd A.; Li, Xiaoyuan; Sun, Li; Wei, Chung Chen; Shirazian, Shahrzad; Liang, Congxin; Vojkovsky, Tomas; Nematalla, Asaad S.; Hawley, Michael
Patent: US2002/156292 A1, 2002 ;
反应条件
1: 5-fluoro-1-(trimethylsilyl)-2-(trimethylsilyloxy)-1H-indole With 1,1,1,3,3,3-hexamethyl-disilazane in acetonitrile 0.25 h; 2: 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid With trifluorormethanesulfonic acid
参考文献
SCINOPHARM TAIWAN, LTD.; Henscheke, Julian P.; Chen, Yung-Fa
Patent: US2013/190512 A1, 2013 ;
Location in patent: Paragraph 0087 ;
反应条件
hydrogenchloride in ethanol 6 h; Reflux;
参考文献
WO2010/1167 A2, ;
Page/Page column 49-50 ;
参考文献
US2003/130280 A1, ;
US 20030130280 A1
反应条件
1: ammonium sulfate / Inert atmosphere; Reflux 2: 1,1,1,3,3,3-hexamethyl-disilazane / trifluorormethanesulfonic acid / acetonitrile / 48 h / 20 - 65 °C View Scheme
反应条件
1: 93 percent / aq. KOH / methanol 2: piperidine / ethanol / 60 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 46, # 7 p. 1116 - 1119
反应条件
1: 64 percent / TFA 2: 93 percent / aq. KOH / methanol 3: piperidine / ethanol / 60 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 46, # 7 p. 1116 - 1119
反应条件
1.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0.17 h 1.2: 25 °C 2.1: N,N-dimethyl-formamide / 25 °C 3.1: methanol / 8 h / 25 °C / Inert atmosphere View Scheme
参考文献
SCINOPHARM TAIWAN, LTD.; Henscheke, Julian P.; Chen, Yung-Fa
Patent: US2013/190512 A1, 2013 ;
