2-氨基-5-甲基-噻吩-3-甲酸乙酯合成路线 (共 8 条)
反应条件
octasulfur; triethylamine in DMF (N,N-dimethyl-formamide); ethanol T=20 - 60°C;
参考文献
Nihon Nohyaku Co., Ltd.
Patent: EP1544202 A1, 2005 ;
Location in patent: Page/Page column 53-54 ;
反应条件
morpholine; sulfur in ethanol 2 h; Heating / reflux;
参考文献
Iyengar, Rajesh R.; Judd, Andrew S.; Zhao, Gang; Kym, Philip R.; Sham, Hing L.; Gu, Yugui; Liu, Gang; Liu, Mei; Zhao, Hongyu; Clark, Richard F.; Frevert, Ernst U.; Cool, Barbara L.; Zhang, Tianyuan; Keyes, Robert F.; Hansen, Todd M.; Xin, Zhili
Patent: US2005/38068 A1, 2005 ;
Location in patent: Page/Page column 47 ;
US 20050038068 A1
反应条件
1: 73 percent / 2 h / Heating 2: 82 percent / phosphorus oxychloride, DMF / 1,2-dichloro-ethane / 1.5 h / Heating 3: 55 percent / N-bromosuccinimide, benzoylperoxide / CCl4 / 1.5 h / Heating View Scheme
参考文献
Kaplina, N. V.; Grinev, A. N.; Bogdanova, G. A.; Alekseeva, L. M.; Pushkina, T. V.; et al.
Pharmaceutical Chemistry Journal, 1987 , vol. 21, # 2 p. 126 - 129
Khimiko-Farmatsevticheskii Zhurnal, 1987 , vol. 21, # 2 p. 197 - 200
参考文献
Kaplina, N. V.; Grinev, A. N.; Bogdanova, G. A.; Alekseeva, L. M.; Pushkina, T. V.; et al.
Pharmaceutical Chemistry Journal, 1987 , vol. 21, # 2 p. 126 - 129
Khimiko-Farmatsevticheskii Zhurnal, 1987 , vol. 21, # 2 p. 197 - 200
反应条件
1: 73 percent / 2 h / Heating 2: 82 percent / phosphorus oxychloride, DMF / 1,2-dichloro-ethane / 1.5 h / Heating View Scheme
参考文献
Golub, Andriy G.; Bdzhola, Volodymyr G.; Briukhovetska, Nadiia V.; Balanda, Anatoliy O.; Kukharenko, Olexander P.; Kotey, Igor M.; Ostrynska, Olga V.; Yarmoluk, Sergiy M.
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 3 p. 870 - 876
反应条件
1: 87 percent / acetic acid / 0.13 h / 110 °C 2: 90 percent / KOH / ethanol; H2O / 1 h / Heating View Scheme
参考文献
Bauer; Heisler; Konigstein
Tetrahedron, 1993 , vol. 49, # 30 p. 6591 - 6604
反应条件
1: With hydrogenchloride in 1,4-dioxane
6 h;
2: With ammonia in 1,4-dioxane; water
参考文献
N.V. Organon
Patent: US2009/131455 A1, 2009 ;
Location in patent: Page/Page column 8 ;
US 20090131455 A1
反应条件
1: 24 h / 160 - 170 °C
2: phosphorus pentachloride; trichlorophosphate
3: potassium carbonate / N,N-dimethyl-formamide / 0.17 h / Heating
View Scheme
参考文献
Golub, Andriy G.; Bdzhola, Volodymyr G.; Briukhovetska, Nadiia V.; Balanda, Anatoliy O.; Kukharenko, Olexander P.; Kotey, Igor M.; Ostrynska, Olga V.; Yarmoluk, Sergiy M.
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 3 p. 870 - 876