3-(三氟甲基)吡唑-4-甲酸乙酯合成路线 （共 14 条）
反应条件
hydrazine hydrate in ethanol T=0 - 20°C; 4.5 h;
参考文献
Guillou, Sandrine; Bonhomme, Frederic J.; Ermolenko, Mikhail S.; Janin, Yves L.
Tetrahedron, 2011 , vol. 67, # 44 p. 8451 - 8457
反应条件
1: With acetic anhydride T=120 - 140°C; 7 h; 2: With hydrazine hydrate in methanol 3 h; Reflux;
参考文献
Nakada, Yoshihisa; Aicher, Thomas D.; Huerou, Yvan Le; Turner, Timothy; Pratt, Scott A.; Gonzales, Stephen S.; Boyd, Steve A.; Miki, Hiroshi; Yamamoto, Toshihiro; Yamaguchi, Hiroshi; Kato, Koki; Kitamura, Shuji
Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 7 p. 2785 - 2795
反应条件
1: With acetic anhydride; orthoformic acid triethyl ester T=120°C; 7 h; Heating / reflux; 2: With hydrazine in methanol; water 3 h; Heating / reflux;
参考文献
WO2006/82952 A1, ;
Page/Page column 174-175 ;
反应条件
sodium hydroxide in ethanol; water 72 h; Heating / reflux;
参考文献
SMITHKLINE BEECHAM CORPORATION
Patent: WO2004/54974 A2, 2004 ;
Location in patent: Page 452 ;
WO 2004/054974 A2
反应条件
trans-N,N'-dimethyl-1,2-cyclohexanediamine; copper(l) iodide; potassium carbonate in toluene T=110°C; 24 h;
参考文献
Bolin, David Robert; Cheung, Adrian Wai-Hing; Firooznia, Fariborz; Marcopulos, Nicholas; Qian, Yimin
Patent: US2010/152445 A1, 2010 ;
Location in patent: Page/Page column 8 ;
反应条件
pyridine; copper diacetate in N,N-dimethyl-formamide T=20°C; 24 h;
参考文献
Wu, Zhibing; Hu, Deyu; Kuang, Jiqing; Cai, Hua; Wu, Shixi; Xue, Wei
Molecules, 2012 , vol. 17, # 12 p. 14205 - 14218
反应条件
1: With lithium aluminium tetrahydride in tetrahydrofuran T=10 - 20°C; 4.5 h; Cooling with acetone/ice bath; 2: With hydrogenchloride; water T=20°C; pH=6;
参考文献
US2009/131455 A1, ;
Page/Page column 7-8 ;
US 20090131455 A1
反应条件
pyridine; sodium hydroxide; copper diacetate in ethanol (100 mL)-THF; N,N-dimethyl-formamide
参考文献
Takeda Pharmaceutical Company Limited
Patent: EP1845081 A1, 2007 ;
EP 1845081 A1
反应条件
1: With pyridine; copper diacetate in N,N-dimethyl-formamide T=20°C; 24 h; 2: With water; sodium hydroxide in tetrahydrofuran; ethanol T=20 - 50°C; 8 h; Heating / reflux; 3: With hydrogenchloride; water
参考文献
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Patent: WO2006/82952 A1, 2006 ;
Location in patent: Page/Page column 175-176 ;
反应条件
1: copper diacetate; pyridine / N,N-dimethyl-formamide / 24 h / 20 °C 2: lithium hydroxide hydrate / tetrahydrofuran / 2 h / 70 °C / pH 5 View Scheme
参考文献
Wu, Zhibing; Hu, Deyu; Kuang, Jiqing; Cai, Hua; Wu, Shixi; Xue, Wei
Molecules, 2012 , vol. 17, # 12 p. 14205 - 14218
