5-氯-3-甲酰基-1H-吲哚-2-羧酸乙酯合成路线 （共 5 条）
反应条件
1.1: triethylsilane; trifluoroacetic acid / 20 °C 2.1: sodium hydroxide / ethanol / 60 °C 2.2: pH 2 View Scheme
参考文献
Piscitelli, Francesco; Ligresti, Alessia; La Regina, Giuseppe; Coluccia, Antonio; Morera, Ludovica; Allara, Marco; Novellino, Ettore; Di Marzo, Vincenzo; Silvestri, Romano
Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5627 - 5631
反应条件
1: N-methyl-N-formyl-aniline With trichlorophosphate
0.25 h;
2: ethyl 5-chloro-1H-indole-2-carboxylate in 1,2-dichloro-ethane
1 h; Heating / reflux;
3: sodium acetate in water; 1,2-dichloro-ethane
T=0°C; 18 h;
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: EP1577301 A1, 2005 ;
Location in patent: Page/Page column 213 ;
反应条件
1: N-methyl-N-formyl-aniline With trichlorophosphate
Vilsmeier formylation; 0.25 h;
2: ethyl 5-chloro-1H-indole-2-carboxylate in 1,2-dichloro-ethane
Vilsmeier formylation; 1 h; Reflux;
参考文献
Yoshikawa, Kenji; Yokomizo, Aki; Naito, Hiroyuki; Haginoya, Noriyasu; Kobayashi, Shozo; Yoshino, Toshiharu; Nagata, Tsutomu; Mochizuki, Akiyoshi; Osanai, Ken; Watanabe, Kengo; Kanno, Hideyuki; Ohta, Toshiharu
Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 24 p. 8206 - 8220
反应条件
sodium acetate; trichlorophosphate
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: US2005/20645 A1, 2005 ;
反应条件
1: With trichlorophosphate
Vilsmeier-Haack reaction; Heating;
2: With water
Vilsmeier-Haack reaction;
参考文献
Piscitelli, Francesco; Ligresti, Alessia; La Regina, Giuseppe; Coluccia, Antonio; Morera, Ludovica; Allara, Marco; Novellino, Ettore; Di Marzo, Vincenzo; Silvestri, Romano
Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5627 - 5631
