5-氯吡嗪-2-羧酸甲酯合成路线 （共 29 条）
反应条件
trimethylaluminum; ammonium chloride in toluene; benzene T=0 - 50°C;
参考文献
R-tech Ueno, Ltd.
Patent: WO2009/145360 A1, 2009 ;
Location in patent: Page/Page column 71 ;
WO 2009/145360 A1
反应条件
1: With water; sodium hydroxide T=20°C; 5 h; 2: With hydrogenchloride in water
参考文献
US2010/93999 A1, ;
Page/Page column 91 ;
US 20100093999 A1
反应条件
1.1: 2.17 h / 0 - 20 °C 2.1: water; lithium hydroxide hydrate / 1,4-dioxane / 24 h / 20 °C 2.2: pH 2 View Scheme
参考文献
WO2011/9898 A1, ;
WO 2011/009898 A1
反应条件
1: 6 percent / MCPBA / 1,2-dichloro-ethane / 39 h / 65 °C
2: 10 percent / NaOH / H2O / 5 h / 70 - 80 °C
View Scheme
参考文献
Mano; Seo; Iami
Chemical and Pharmaceutical Bulletin, 1980 , vol. 28, # 10 p. 3057 - 3063
反应条件
1: With diisobutylaluminium hydride in tetrahydrofuran; hexane
T=-70 - -60°C; 1.33333 h; Inert atmosphere;
2: With ammonium chloride in tetrahydrofuran; hexane; water
参考文献
MITSUBISHI TANABE PHARMA CORPORATION; SAKURAI, Osamu; SARUTA, Kunio; HAYASHI, Norimitsu; GOI, Takashi; MOROKUMA, Kenji; TSUJISHIMA, Hidekazu; SAWAMOTO, Hiroaki; SHITAMA, Hiroaki; IMASHIRO, Ritsuo
Patent: WO2012/81736 A1, 2012 ;
Location in patent: Page/Page column 91-92 ;
WO 2012/081736 A1
反应条件
bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide; triethylamine
T=50°C; 24 h;
参考文献
Yamanaka; Mizugaki; Sakamoto; et al.
Chemical and Pharmaceutical Bulletin, 1983 , vol. 31, # 12 p. 4549 - 4553
反应条件
1: 76 percent / Pd(PPh3)2Cl2/CuI/Et3N / 24 h / 50 °C
2: 94 percent / H2 / 5percent Pd-charcoal / methanol
View Scheme
参考文献
Yamanaka; Mizugaki; Sakamoto; et al.
Chemical and Pharmaceutical Bulletin, 1983 , vol. 31, # 12 p. 4549 - 4553
反应条件
1: 76 percent / Pd(PPh3)2Cl2/CuI/Et3N / 24 h / 50 °C
2: 94 percent / H2 / 5percent Pd-charcoal / methanol
3: 3N NaOH / Ambient temperature; pH: 2.6
View Scheme
参考文献
Yamanaka; Mizugaki; Sakamoto; et al.
Chemical and Pharmaceutical Bulletin, 1983 , vol. 31, # 12 p. 4549 - 4553
反应条件
triethylamine in tetrahydrofuran
T=20°C; 2 h;
参考文献
MERCK and CO., INC.
Patent: WO2007/81897 A2, 2007 ;
Location in patent: Page/Page column 29 ;
WO 2007/081897 A2
