3-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)h-吡唑并[1,5-a]吡啶合成路线 (共 7 条)
反应条件
isopropylmagnesium chloride lithium chloride complex in tetrahydrofuran T=5 - 10°C; 2 h; Inert atmosphere;
参考文献
Bethel, Paul A.; Campbell, Andrew D.; Goldberg, Frederick W.; Kemmitt, Paul D.; Lamont, Gillian M.; Suleman, Abid
Tetrahedron, 2012 , vol. 68, # 27-28 p. 5434 - 5444
反应条件
potassium carbonate; tri-cyclo-hexyl-phosphine; palladium diacetate in diethylene glycol dimethyl ether; water T=100°C; Suzuki-Miyaura reaction; 2 h;
参考文献
ALMIRALL, S.A.; BACH TANA, Jordi; PAGES SANTACANA, Lluis, Miquel; TALTAVULL MOLL, Joan; EASTWOOD, Paul, Robert; GONZALEZ RODRIGUES, Jacob; GIULIO MATASSA, Victor
Patent: WO2011/101161 A1, 2011 ;
Location in patent: Page/Page column 103 ;
WO 2011/101161 A1
反应条件
n-butyllithium in tetrahydrofuran T=-78 - 20°C;
参考文献
MERCK and CO., INC.; KATZ, Jason; KNOWLES, Sandra, L.; JEWELL, James, P.; SLOMAN, David, L.; STANTON, Matthew, G.; NOUCTI, Njamkou
Patent: WO2010/17046 A1, 2010 ;
Location in patent: Page/Page column 47; 126-127 ;
WO 2010/017046 A1
反应条件
1: sodium hydroxide; water / ethanol / 1 h / Reflux 2: sodium hydrogencarbonate; N-bromosuccinmide / N,N-dimethyl-formamide / 4 h / 20 °C 3: potassium carbonate; tri-cyclo-hexyl-phosphine / palladium diacetate / water; diethylene glycol dimethyl ether / 2 h / 100 °C View Scheme
参考文献
Bethel, Paul A.; Campbell, Andrew D.; Goldberg, Frederick W.; Kemmitt, Paul D.; Lamont, Gillian M.; Suleman, Abid
Tetrahedron, 2012 , vol. 68, # 27-28 p. 5434 - 5444
反应条件
1: sodium hydrogencarbonate; N-bromosuccinmide / N,N-dimethyl-formamide / 4 h / 20 °C 2: potassium carbonate; tri-cyclo-hexyl-phosphine / palladium diacetate / water; diethylene glycol dimethyl ether / 2 h / 100 °C View Scheme
参考文献
Bethel, Paul A.; Campbell, Andrew D.; Goldberg, Frederick W.; Kemmitt, Paul D.; Lamont, Gillian M.; Suleman, Abid
Tetrahedron, 2012 , vol. 68, # 27-28 p. 5434 - 5444
反应条件
1: N-iodo-succinimide / acetonitrile / 1 h / 20 °C 2: isopropylmagnesium chloride lithium chloride complex / tetrahydrofuran / 2 h / 5 - 10 °C / Inert atmosphere View Scheme
参考文献
Bethel, Paul A.; Campbell, Andrew D.; Goldberg, Frederick W.; Kemmitt, Paul D.; Lamont, Gillian M.; Suleman, Abid
Tetrahedron, 2012 , vol. 68, # 27-28 p. 5434 - 5444
反应条件
mono(bis(di-tert-butyl(4-(dimethylamino)phenyl)phosphonio)palladium(II))dichloride; water; sodium carbonate in ethylene glycol dimethyl ether T=85°C; Suzuki coupling; 3 h; Inert atmosphere;
参考文献
Bethel, Paul A.; Campbell, Andrew D.; Goldberg, Frederick W.; Kemmitt, Paul D.; Lamont, Gillian M.; Suleman, Abid
Tetrahedron, 2012 , vol. 68, # 27-28 p. 5434 - 5444