5-氯吲哚-2-羧酸乙酯合成路线 （共 37 条）
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
反应条件
1.1: AlCl3, aluminium chloride / 1,2-dichloro-ethane / Reflux
2.1: triethylsilane; trifluoroacetic acid / 20 °C
3.1: sodium hydroxide / ethanol / 60 °C
3.2: pH 2
View Scheme
参考文献
Mahmoud, Mariam M.; Ali, Hamed I.; Ahn, Kwang H.; Damaraju, Aparna; Samala, Sushma; Pulipati, Venkata K.; Kolluru, Srikanth; Kendall, Debra A.; Lu, Dai
Journal of Medicinal Chemistry, 2013 , vol. 56, # 20 p. 7965 - 7975
反应条件
1: BF3*Et2O / CH2Cl2 / 4 h / 20 - 45 °C
2: MCPBA / CHCl3 / 1 h / 20 °C
3: 94 percent / aq. LiOH / tetrahydrofuran / 24 h / 20 °C
View Scheme
参考文献
Silvestri, Romano; Artico, Marino; De Martino, Gabriella; La Regina, Giuseppe; Loddo, Roberta; La Colla, Massimiliano; La Colla, Paolo
Journal of Medicinal Chemistry, 2004 , vol. 47, # 15 p. 3892 - 3896
参考文献
Synthelabo
Patent: US6075021 A1, 2000 ;
反应条件
sodium hydroxide; tetrabutylammomium bromide in diethyl ether
6 h; Ambient temperature;
参考文献
Lehr, Matthias
Journal of Medicinal Chemistry, 1997 , vol. 40, # 17 p. 2694 - 2705
