1-乙酰基-1H-噻吩并[3,2-c]吡唑-5-羧酸甲酯合成路线 （共 7 条）
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: nitric acid; sulfuric acid / 0.5 h / 0 °C
2.1: hydrogen / Raney Ni / tetrahydrofuran; methanol / 36 h / 20 °C / 760.05 Torr
3.1: potassium acetate / toluene / 3 h / 100 °C
3.2: 100 °C
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
1.1: sulfuric acid / 60 h / Reflux
2.1: nitric acid; sulfuric acid / 0.5 h / 0 °C
3.1: hydrogen / Raney Ni / tetrahydrofuran; methanol / 36 h / 20 °C / 760.05 Torr
4.1: potassium acetate / toluene / 3 h / 100 °C
4.2: 100 °C
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
1.1: hydrogen / Raney Ni / tetrahydrofuran; methanol / 36 h / 20 °C / 760.05 Torr
2.1: potassium acetate / toluene / 3 h / 100 °C
2.2: 100 °C
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 sodium tetrahydroborate in methanol
T=20°C; 0.5 h;
2: With lithium aluminium tetrahydride in tetrahydrofuran
T=0°C; 0.5 h;
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
