1-[(4-甲氧基苯基)甲基]-1H-吡唑-5-胺合成路线 （共 7 条）
反应条件
1: acrylonitrile With hydrazine in tetrahydrofuran; water T=0 - 20°C; 2.33 h; 2: 4-methoxy-benzaldehyde in tetrahydrofuran; water 3.25 h; 3: With sodium n-butanolate in butan-1-ol T=25 - 120°C; 3.33 h;
参考文献
GENENTECH, INC.; FORMA TM, LLC; BAIR, Kenneth W.; BAUMEISTER, Timm R.; DRAGOVICH, Peter; GOSSELIN, Francis; YUEN, Po-Wai; ZAK, Mark; ZHENG, Xiaozhang
Patent: WO2013/127267 A1, 2013 ;
Location in patent: Page/Page column 83 ;
反应条件
1: hydrazine hydrate; acrylonitrile in tetrahydrofuran T=0 - 20°C; 1.25 h; 2: 4-methoxy-benzaldehyde T=20°C; 17 h; 3: With potassium tert-butylate in butan-1-ol T=20 - 120°C; 18.5 h; Sealed tube;
参考文献
AMBIT BIOSCIENCES CORPORATION; FARAONI, Raffaella; HADD, Michael, J.; HOLLADAY, Mark, W.; ROWBOTTOM, Martin; SETTI, Eduardo
Patent: WO2012/30944 A2, 2012 ;
Location in patent: Page/Page column 95-96 ;
WO 2012/030944 A2
反应条件
sodium hydroxide in tert-butyl methyl ether; water Product distribution / selectivity;
参考文献
Bristol-Myers Squibb Company
Patent: EP1043998 B1, 2007 ;
Location in patent: Page/Page column 13 ;
反应条件
sodium t-butanolate in isopropyl alcohol T=110°C; 4 h;
参考文献
US2011/86889 A1, ;
Page/Page column 12 ;
反应条件
1: in ethanol T=70°C; 2 h; 2: With sodium t-butanolate in isopropyl alcohol T=110°C; 4 h; 3: With hydrogenchloride in diethyl ether; water
参考文献
WO2009/150614 A1, ;
Page/Page column 31 ;
WO 2009/150614 A1
反应条件
1: acrylonitrile With hydrazine hydrate in tetrahydrofuran T=0 - 25°C; 2 h; 2: 4-methyl-benzaldehyde in tetrahydrofuran T=25°C; 2 h; 3: With sodium n-butanolate; butan-1-ol T=120°C; 3 h;
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 13, # 6 p. 1133 - 1136
反应条件
1: ethanol / 2 h / 70 °C 2: sodium t-butanolate / isopropyl alcohol / 4 h / 110 °C View Scheme
