1-(4-甲氧基苄基)-3-甲基-1H-吡唑-5-胺合成路线 (共 4 条)
反应条件
1: (E,Z)-crotononitrile With hydrazine in tetrahydrofuran; water
T=0 - 20°C; 2.33 h;
2: 4-methoxy-benzaldehyde in tetrahydrofuran; water
T=20°C; 3.25 h;
3: With sodium n-butanolate in butan-1-ol
T=25 - 120°C; 3.33 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GmbH
Patent: WO2009/62308 A1, 2009 ;
Location in patent: Page/Page column 56-58 ;
反应条件
1: methyl acetate; acetonitrile With potassium tert-butylate in tetrahydrofuran
T=5 - 20°C;
2: (4-methoxybenzyl)hydrazine dihydrochloride in tetrahydrofuran
0.0833333 h;
参考文献
ELI LILLY AND COMPANY
Patent: US2010/152181 A1, 2010 ;
Location in patent: Page/Page column 2 ;
反应条件
hydrogenchloride in 1,4-dioxane
Reflux;
参考文献
Mitchell, David; Cole, Kevin P.; Pollock, Patrick M.; Coppert, David M.; Burkholder, Timothy P.; Clayton, Joshua R.
Organic Process Research and Development, 2012 , vol. 16, # 1 p. 70 - 81
反应条件
1: ethanol / Reflux
2: 10 palladium on activated charcoal; hydrogen / ethanol / 10 - 20 °C / 775.74 Torr
3: hydrogenchloride / methanol / 40 - 60 °C
4: hydrogenchloride / 1,4-dioxane / Reflux
View Scheme
参考文献
Mitchell, David; Cole, Kevin P.; Pollock, Patrick M.; Coppert, David M.; Burkholder, Timothy P.; Clayton, Joshua R.
Organic Process Research and Development, 2012 , vol. 16, # 1 p. 70 - 81