2-氨基-3,5-二溴吡嗪合成路线 (共 54 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
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: sodium cyanide; copper (I) cyanide in N,N-dimethyl-formamide T=125°C; 2: 3,5-dibromopyrazine-2-ylamine in N,N-dimethyl-formamide T=125°C; 5 h;
参考文献
Folmer, Brigitte Johanna Bernita; Man, de Adrianus Petrus Antonius; Gernette, Elisabeth Sophia; Corte Real Goncalves Azevedo, Rita; Ibrahim, Hemen
Patent: US2013/79341 A1, 2013 ;
Location in patent: Paragraph 0119 ;
反应条件
copper(l) iodide; 18-crown-6 ether; tetrakis(triphenylphosphine) palladium(0) in N,N-dimethyl-formamide 1 h; Heating;
参考文献
Journal of Heterocyclic Chemistry, , vol. 24, p. 1371 - 1372
反应条件
in N,N-dimethyl-formamide T=120 - 130°C; 2.5 h;
参考文献
Synthesis, , # 8 p. 659 - 660
反应条件
1: With hydrogenchloride; isopentyl nitrite T=60°C; 2 h; 2: With sodium hydrogencarbonate in dichloromethane; water
参考文献
KALYPSYS, INC.; BORCHARDT, Allen; DAVIS, Robert; NOBLE, Stewart, A.
Patent: WO2011/112766 A2, 2011 ;
Location in patent: Page/Page column 71; 72 ;
反应条件
sodium ethanolate in N,N-dimethyl-formamide T=90°C; 2 h;
参考文献
Sablayrolles, C.; Constantin, A.; Ducourant, B.; Fruchier, A.; Chapat, J.-P.
Bulletin de la Societe Chimique de France, 1989 , # 4 p. 467 - 471
反应条件
copper(l) iodide; 18-crown-6 ether; tetrakis(triphenylphosphine) palladium(0) in N,N-dimethyl-formamide
1 h; Heating;
参考文献
Sato, Nobuhiro; Suzuki, Masakazu
Journal of Heterocyclic Chemistry, 1987 , vol. 24, p. 1371 - 1372
反应条件
in N,N-dimethyl-formamide
T=120 - 130°C; 2.5 h;
参考文献
Sato, Nobuhiro; Takeuchi, Ryo
Synthesis, 1990 , # 8 p. 659 - 660
反应条件
copper in methanol
T=140°C; 16 h; Sealed tube;
参考文献
MEDEIA THERAPEUTICS LTD; GOLDSTEINS, Gundars; KOISTINAHO, Jari; KOISTINAHO, Milla; RATILAINEN, Jari; PYSTYNEN, Jarmo
Patent: WO2014/68171 A1, 2014 ;
Location in patent: Page/Page column 29 ;