4-氨基-5-甲基噻吩-2-羧酸甲酯合成路线 （共 8 条）
反应条件
hydrogen; palladium 10 on activated carbon in ethyl acetate
P=2585.81 Torr;
参考文献
AVENTIS PHARMACEUTICALS INC.
Patent: WO2005/26175 A1, 2005 ;
Location in patent: Page/Page column 75-76 ;
WO 2005/026175 A1
参考文献
Sorenson, Roderick Joseph
Patent: US2003/87924 A1, 2003 ;
US 20030087924 A1
反应条件
1: nitric acid; sulfuric acid / 0.5 h / 0 °C
2: hydrogen / Raney Ni / tetrahydrofuran; methanol / 36 h / 20 °C / 760.05 Torr
View Scheme
参考文献
HUTCHISON MEDIPHARMA LIMITED; SU, Wei-Guo; JIA, Hong; DAI, Guangxiu
Patent: WO2011/79804 A1, 2011 ;
WO 2011/079804 A1
反应条件
1: sulfuric acid / 60 h / Reflux
2: nitric acid; sulfuric acid / 0.5 h / 0 °C
3: hydrogen / Raney Ni / tetrahydrofuran; methanol / 36 h / 20 °C / 760.05 Torr
View Scheme
参考文献
HUTCHISON MEDIPHARMA LIMITED; SU, Wei-Guo; JIA, Hong; DAI, Guangxiu
Patent: WO2011/79804 A1, 2011 ;
WO 2011/079804 A1
反应条件
1: With potassium acetate in toluene
2: With isopentyl nitrite in toluene
T=93°C;
参考文献
AVENTIS PHARMACEUTICALS INC.
Patent: WO2005/26175 A1, 2005 ;
Location in patent: Page/Page column 75-76 ;
WO 2005/026175 A1
反应条件
1: With acetic anhydride in toluene
T=93°C;
2: With isopentyl nitrite in toluene
T=93°C; 12 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO KG
Patent: WO2007/76228 A2, 2007 ;
Location in patent: Page/Page column 24 ;
WO 2007/076228 A2
反应条件
1: 5-methyl-4-amino-thiophene-2-carboxylic acid methyl ester With potassium acetate; acetic anhydride in toluene
T=100°C; 3 h;
2: iso-butyl nitrite in toluene
T=100°C;
参考文献
SU, Wei-Guo; JIA, Hong; DAI, Guangxiu
Patent: US2012/245178 A1, 2012 ;
Location in patent: Page/Page column 16 ;
US 20120245178 A1
反应条件
1.1: potassium acetate / toluene / 3 h / 100 °C
1.2: 100 °C
2.1: sodium tetrahydroborate / methanol / 0.5 h / 20 °C
2.2: 0.5 h / 0 °C
View Scheme
参考文献
SU, Wei-Guo; JIA, Hong; DAI, Guangxiu
Patent: US2012/245178 A1, 2012 ;
US 20120245178 A1
