2-氨基-3-(苯基甲基)-5-溴吡嗪合成路线 （共 10 条）
反应条件
1: benzyl bromide With iodine; zinc in N,N-dimethyl acetamide T=80°C; 3 h; Inert atmosphere; 2: 3,5-dibromopyrazine-2-ylamine With bis-triphenylphosphine-palladium(II) chloride in N,N-dimethyl acetamide Negishi Coupling; 120 h; Inert atmosphere;
参考文献
Shrestha, Tej B.; Troyer, Deryl L.; Bossmann, Stefan H.
Synthesis (Germany), 2014 , vol. 46, # 5 art. no. 673, p. 646 - 652
反应条件
pyridine; tetra-n-butylammonium tribromide in chloroform T=20°C; 0.75 h;
参考文献
Adamczyk, Maciej; Johnson, Donald D.; Mattingly, Phillip G.; Pan, You; Reddy, Rajarathnam E.
Organic Preparations and Procedures International, 2001 , vol. 33, # 5 p. 477 - 485
反应条件
1: chloro(phenylmethyl)-magnesium With zinc(II) chloride in tetrahydrofuran; diethyl ether T=20°C; 0.25 h; 2: 3,5-dibromopyrazine-2-ylamine With bis-triphenylphosphine-palladium(II) chloride in tetrahydrofuran; diethyl ether T=20°C; 54 h;
参考文献
Adamczyk, Maciej; Akireddy, Srinivasa Rao; Johnson, Donald D.; Mattingly, Phillip G.; Pan, You; Reddy, Rajarathnam E.
Tetrahedron, 2003 , vol. 59, # 41 p. 8129 - 8142
反应条件
1.1: n-BuLi; TMEDA / hexane / 0.5 h / Heating 1.2: 44 percent / hexane; tetrahydrofuran / 0.5 h / 0 °C 2.1: 89 percent / tetra-n-butylammonium tribromide; pyridine / CHCl3 / 0.75 h / 20 °C View Scheme
参考文献
UNIVERSITA DEGLI STUDI DI SIENA; GIULIANI, Germano; CAPPELLI, Andrea; VOMERO, Salvatore; ANZINI, Maurizio
Patent: WO2011/7314 A1, 2011 ;
反应条件
1: 98 percent / 1,4-bis(diphenylphospino)butane; (PhCN)2PdCl2; Na2CO3 / toluene; ethanol; H2O / 0.12 h / Heating 2: 63 percent / HCl / H2O; dioxane / 5 h / Heating View Scheme
参考文献
Adamczyk, Maciej; Akireddy, Srinivasa Rao; Johnson, Donald D.; Mattingly, Phillip G.; Pan, You; Reddy, Rajarathnam E.
Tetrahedron, 2003 , vol. 59, # 41 p. 8129 - 8142
反应条件
1.1: n-butyllithium / tetrahydrofuran; hexane / 1 h / -78 °C 1.2: 1.5 h / -78 - 20 °C 1.3: 20 °C 2.1: hydrogenchloride / ethanol; water / 8 h / |Inert atmosphere; |Reflux View Scheme
参考文献
Shrestha, Tej B.; Troyer, Deryl L.; Bossmann, Stefan H.
Synthesis (Germany), 2014 , vol. 46, # 5 art. no. 673, p. 646 - 652
反应条件
1: caesium carbonate / palladium diacetate; 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl / toluene; ethanol / Inert atmosphere; Reflux 2: hydrogenchloride / ethanol; water / Reflux View Scheme
参考文献
UNIVERSITA DEGLI STUDI DI SIENA; GIULIANI, Germano; CAPPELLI, Andrea; VOMERO, Salvatore; ANZINI, Maurizio
Patent: WO2011/7314 A1, 2011 ;
反应条件
1: 88 percent / (PhCN)2PdCl2; 1,4-bis(diphenylphosphino)butane; Na2CO3 / toluene; ethanol; H2O / 4 h / Heating
2: 75 percent / pyridine hydrochloride / 0.5 h / Heating
View Scheme
参考文献
UNIVERSITA DEGLI STUDI DI SIENA; GIULIANI, Germano; CAPPELLI, Andrea; VOMERO, Salvatore; ANZINI, Maurizio
Patent: WO2011/7314 A1, 2011 ;
反应条件
sodium carbonate; [1,4-bis-(diphenylphosphine)butane]palladium (II) dichloride in ethylene glycol dimethyl ether; ethanol; water
T=90°C; 2.5 h; Inert atmosphere;
参考文献
TOKYO INSTITUTE OF TECHNOLOGY; JNC CORPORATION
Patent: US2011/288280 A1, 2011 ;
Location in patent: Page/Page column 36 ;
反应条件
bis(benzonitrile)palladium(II) dichloride; sodium carbonate; 1,4-di(diphenylphosphino)-butane in ethanol; water; toluene
4 h; Heating;
参考文献
Adamczyk, Maciej; Johnson, Donald D.; Mattingly, Phillip G.; Pan, You; Reddy, Rajarathnam E.
Organic Preparations and Procedures International, 2001 , vol. 33, # 5 p. 477 - 485
