1H-噻吩并[3,2-c]吡唑-5-基甲醇合成路线 （共 5 条）
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
HUTCHISON MEDIPHARMA LIMITED; SU, Wei-Guo; JIA, Hong; DAI, Guangxiu
Patent: WO2011/79804 A1, 2011 ;
Location in patent: Page/Page column 30 ;
WO 2011/079804 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
4.1: sodium tetrahydroborate / methanol / 0.5 h / 20 °C
4.2: 0.5 h / 0 °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
5.1: sodium tetrahydroborate / methanol / 0.5 h / 20 °C
5.2: 0.5 h / 0 °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
3.1: sodium tetrahydroborate / methanol / 0.5 h / 20 °C
3.2: 0.5 h / 0 °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: 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
HUTCHISON MEDIPHARMA LIMITED; SU, Wei-Guo; JIA, Hong; DAI, Guangxiu
Patent: WO2011/79804 A1, 2011 ;
WO 2011/079804 A1
