3-氨基-6-溴吡嗪-2-甲酸合成路线 (共 7 条)
反应条件
1: With water; lithium hydroxide hydrate in methanol T=90°C; 5 h; 2: With hydrogenchloride in methanol; water
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; CHARRIER, Jean-Damien; DURRANT, Steven, John; KNEGTEL, Ronald, Marcellus, Alphonsus; O'DONNELL, Michael; REAPER, Philip, Michael
Patent: WO2011/143419 A1, 2011 ;
Location in patent: Page/Page column 44-45 ;
WO 2011/143419 A1
反应条件
1: bromine 2: aq. NaOH solution View Scheme
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED; FENG, Tao; SANGANEE, Hitesh, Jayantilal; WADA, Hiroki
Patent: WO2011/89416 A1, 2011 ;
WO 2011/089416 A1
反应条件
1: sulfuric acid 2: bromine; acetic acid 3: sodium hydroxide / ethanol View Scheme
参考文献
Forns, Pilar; Esteve, Cristina; Taboada, Lorena; Alonso, Juan Antonio; Orellana, Adelina; Maldonado, Monica; Carreno, Cristina; Ramis, Isabel; Lopez, Manel; Miralpeix, Montserrat; Vidal, Bernat
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 8 p. 2784 - 2788
反应条件
1,2,3,4-tetrahydro-naphthalene
参考文献
Ellingson; Henry
Journal of the American Chemical Society, 1949 , vol. 71, p. 2798
反应条件
1.1: 4-(N,N-dimethlyamino)pyridine; N-ethyl-N,N-diisopropylamine; 1,1'-carbonyldiimidazole / dimethyl sulfoxide / 0.5 h 1.2: 18 h / 20 °C 2.1: tetrakis(triphenylphosphine) palladium(0); sodium carbonate / 1,4-dioxane; water / 0.5 h / 150 °C / Microwave irradiation; Inert atmosphere View Scheme
参考文献
Charrier, Jean-Damien; Durrant, Steven J.; Golec, Julian M. C.; Kay, David P.; Knegtel, Ronald M. A.; MacCormick, Somhairle; Mortimore, Michael; O'Donnell, Michael E.; Pinder, Joanne L.; Reaper, Philip M.; Rutherford, Alistair P.; Wang, Paul S. H.; Young, Stephen C.; Pollard, John R.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 7 p. 2320 - 2330
反应条件
sulfuric acid in water
参考文献
Shirude, Pravin S.; Madhavapeddi, Prashanti; Tucker, Julie A.; Murugan, Kannan; Patil, Vikas; Basavarajappa, Halesha; Raichurkar, Anandkumar V.; Humnabadkar, Vaishali; Hussein, Syeed; Sharma, Sreevalli; Ramya; Narayan, Chandan B.; Balganesh, Tanjore S.; Sambandamurthy, Vasan K.
ACS Chemical Biology, 2013 , vol. 8, # 3 p. 519 - 523
反应条件
1.1: 4-(N,N-dimethlyamino)pyridine; N-ethyl-N,N-diisopropylamine; 1,1'-carbonyldiimidazole / dimethyl sulfoxide / 0.5 h 1.2: 18 h / 20 °C 2.1: sodium carbonate / water; N,N-dimethyl-formamide / 18 h / 88 °C / Inert atmosphere View Scheme
参考文献
Charrier, Jean-Damien; Durrant, Steven J.; Golec, Julian M. C.; Kay, David P.; Knegtel, Ronald M. A.; MacCormick, Somhairle; Mortimore, Michael; O'Donnell, Michael E.; Pinder, Joanne L.; Reaper, Philip M.; Rutherford, Alistair P.; Wang, Paul S. H.; Young, Stephen C.; Pollard, John R.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 7 p. 2320 - 2330