5-氨基-1,3-二甲基吡唑合成路线 (共 27 条)
反应条件
1: 89 percent / 1 h / 120 °C 2: 77 percent / POCl3 / 18 h / 120 °C 3: 99 percent / potassium hydroxide / H2O; 1,2-dimethoxy-ethane / 18 h / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 12, # 15 p. 4089 - 4100
反应条件
PdCl(C3H5)(dppb); potassium acetate in N,N-dimethyl acetamide
T=150°C; 20 h; Inert atmosphere;
参考文献
Derridj, Fazia; Roger, Julien; Djebbar, Safia; Doucet, Henri
Advanced Synthesis and Catalysis, 2012 , vol. 354, # 4 p. 747 - 750
反应条件
pyridine
T=0 - 20°C; 0.5 h;
参考文献
REDDY US THERAPEUTICS, INC.; BARUAH, Anima; DE, Dibyendu; KHANNA, Ish Kumar; PILLARISETTI, Sivaram; MAITRA, Santanu; ALEXANDER, Christopher, W.; SREENU, Jennepalli; DAGER, Indu
Patent: WO2006/73973 A2, 2006 ;
Location in patent: Page/Page column 172 ;
反应条件
in ethyl acetate
T=25°C;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2009/153589 A1, 2009 ;
Location in patent: Page/Page column 222 ;
WO 2009/153589 A1
反应条件
1: N-(2,5-dimethyl-2H-pyrazol-3-yl)-amine; acetic anhydride T=90 - 100°C; 4 h;
2: With trichlorophosphate
T=90 - 95°C; 3 h;
3: N,N-dimethyl-formamide T=90 - 95°C; 2.5 h; Product distribution / selectivity;
参考文献
REDDY US THERAPEUTICS, INC.; BARUAH, Anima; DE, Dibyendu; KHANNA, Ish Kumar; PILLARISETTI, Sivaram; MAITRA, Santanu; ALEXANDER, Christopher, W.; SREENU, Jennepalli; DAGER, Indu
Patent: WO2006/73973 A2, 2006 ;
Location in patent: Page/Page column 151-152 ;
反应条件
1: With sodium nitrite in hydrogenchloride
T=0°C;
2: With tin(ll) chloride in hydrogenchloride
T=20°C;
参考文献
Blass, Benjamin E.; Srivastava, Anil; Coburn, Keith R.; Faulkner, Amy L.; Seibel, William L.
Tetrahedron Letters, 2003 , vol. 44, # 14 p. 3009 - 3011
反应条件
1: (i) toluene, (ii) /BRN= 506166/
2: aq. NaOH
View Scheme
参考文献
Swett; Ratajczyk; Nordeen; Aynilian
Journal of Heterocyclic Chemistry, 1975 , vol. 12, # 6 p. 1137 - 1142