5-甲氧基-3-甲基-1H-吲哚-2-羧酸乙酯合成路线 （共 9 条）
反应条件
triethylsilane; trifluoroacetic acid T=20°C; 5 h;
参考文献
Thanigaimalai, Pillaiyar; Konno, Sho; Yamamoto, Takehito; Koiwai, Yuji; Taguchi, Akihiro; Takayama, Kentaro; Yakushiji, Fumika; Akaji, Kenichi; Chen, Shen-En; Naser-Tavakolian, Aurash; Schoen, Arne; Freire, Ernesto; Hayashi, Yoshio
European Journal of Medicinal Chemistry, 2013 , vol. 68, p. 372 - 384
反应条件
1: 4-methoxy-aniline With hydrogenchloride; sodium nitrite in water T=0°C; 0.25 h; 2: 2-ethylacetoacetic acid ethyl ester With potassium hydroxide in ethanol; water T=0 - 4°C; Japp-Klingmann reaction; pH=5 - 6; 15 h; 3: With hydrogenchloride in ethanol T=78°C; Fischer indole synthesis; 2 h;
参考文献
Edwankar, Chitra R.; Edwankar, Rahul V.; Namjoshi, Ojas A.; Liao, Xuebin; Cook, James M.
Journal of Organic Chemistry, 2013 , vol. 78, # 13 p. 6471 - 6487
反应条件
sulfuric acid in ethanol Fischer Indole Synthesis; 16 h; Heating / reflux;
参考文献
AstraZeneca AB
Patent: US6737435 B1, 2004 ;
Location in patent: Page/Page column 21 ;
US 6737435 B1
反应条件
1: trichlorophosphate / N,N-dimethyl-formamide / 2.5 h / 110 °C / |Cooling with ice 2: triethylsilane; trifluoroacetic acid / 5 h / 20 °C View Scheme
参考文献
Thanigaimalai, Pillaiyar; Konno, Sho; Yamamoto, Takehito; Koiwai, Yuji; Taguchi, Akihiro; Takayama, Kentaro; Yakushiji, Fumika; Akaji, Kenichi; Chen, Shen-En; Naser-Tavakolian, Aurash; Schoen, Arne; Freire, Ernesto; Hayashi, Yoshio
European Journal of Medicinal Chemistry, 2013 , vol. 68, p. 372 - 384
反应条件
1: NH2NH2*H2O / ethanol 2: 80 percent / KOH / ethanol; H2O / Heating View Scheme
参考文献
Patil, Renukadevi; Biradar
Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1999 , vol. 38, # 1 p. 76 - 82
反应条件
potassium hydroxide in ethanol 1 h; Heating;
参考文献
Zhao, Shuo; Liao, Xuebin; Wang, Tao; Flippen-Anderson, Judith; Cook, James M.
Journal of Organic Chemistry, 2003 , vol. 68, # 16 p. 6279 - 6295
反应条件
1: 100 percent / KOH / ethanol / 1 h / Heating 2: 93.6 percent / Cu; quinoline / 2.5 h / Heating View Scheme
参考文献
Edwankar, Chitra R.; Edwankar, Rahul V.; Namjoshi, Ojas A.; Liao, Xuebin; Cook, James M.
Journal of Organic Chemistry, 2013 , vol. 78, # 13 p. 6471 - 6487
参考文献
Keimatsu; Sugasawa
Yakugaku Zasshi, 1928 , vol. 48, p. 63
Chem. Zentralbl., 1928 , vol. 99, # II p. 49
反应条件
1: ethyl-5-methoxy-3-methyl-1H-indole-2-carboxylate With sodium hydride in N,N-dimethyl-formamide
T=0°C; 0.666667 h;
2: methyl iodide in N,N-dimethyl-formamide
T=20°C; 2 h; Further stages.;
参考文献
Rigby, James H.; Sidique, Shyama
Organic Letters, 2007 , vol. 9, # 7 p. 1219 - 1221
