3-溴-5-(4-吗啉基)吡啶合成路线 (共 7 条)
反应条件
tris-(dibenzylideneacetone)dipalladium(0); 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl; sodium t-butanolate in toluene T=115°C; 18 h; Inert atmosphere;
参考文献
Bunnelle, William H.; Tietje, Karin R.; Frost, Jennifer M.; Peters, Dan; Ji, Anguo; Li, Tao; Scanio, Marc J. C.; Shi, Lei; Anderson, David J.; Dyhring, Tino; Gronlien, Jens H.; Ween, Hilde; Thorin-Hagene, Kirsten; Meyer, Michael D.
Journal of Medicinal Chemistry, 2009 , vol. 52, # 14 p. 4126 - 4141
反应条件
1: 3.5-Dibromopyridine With isopropylmagnesium chloride lithium chloride complex in tetrahydrofuran T=0 - 25°C; 1.16667 h; Inert atmosphere; 2: With zinc(II) chloride in tetrahydrofuran T=0°C; 0.5 h; Inert atmosphere; 3: lithium (3-oxatetramethylene)amide Further stages;
参考文献
Kienle, Marcel; Dunst, Cora; Knochel, Paul
Organic Letters, 2009 , vol. 11, # 22 p. 5158 - 5161
反应条件
sodium amide; sodium t-butanolate in tetrahydrofuran T=40 - 50°C; 0.75 h;
参考文献
Heterocycles, , vol. 45, # 11 p. 2113 - 2129
反应条件
1.1: diethylamine; n-hexylMgCl / tetrahydrofuran / -78 °C 1.2: -40 - 0 °C 2.1: cesium fluoride View Scheme
参考文献
Nature Chemistry, , vol. 5, # 1 p. 54 - 60
反应条件
1.1: triethylamine / dichloromethane 2.1: N,N,N',N,-tetramethylethylenediamine; t-butyldimethylsiyl triflate / tetrahydrofuran; diethyl ether / -78 - 23 °C 2.2: -78 °C 2.3: -78 °C 3.1: diethylamine; n-hexylMgCl / tetrahydrofuran / -78 °C 3.2: -40 - 0 °C 4.1: cesium fluoride View Scheme
参考文献
Nature Chemistry, , vol. 5, # 1 p. 54 - 60
反应条件
1.1: N,N,N',N,-tetramethylethylenediamine; t-butyldimethylsiyl triflate / tetrahydrofuran; diethyl ether / -78 - 23 °C 1.2: -78 °C 1.3: -78 °C 2.1: diethylamine; n-hexylMgCl / tetrahydrofuran / -78 °C 2.2: -40 - 0 °C 3.1: cesium fluoride View Scheme
参考文献
Nature Chemistry, , vol. 5, # 1 p. 54 - 60
反应条件
cesium fluoride Overall yield = 64 percent; regioselective reaction;
参考文献
Nature Chemistry, , vol. 5, # 1 p. 54 - 60