4,5,6,7-四氢噻吩并[3,2-c]吡啶-2(3H)-酮 4-甲基苯磺酸盐合成路线 （共 6 条）
反应条件
triethylamine in methanol; acetone
参考文献
ZENTIVA, K.S.; STEPANKOVA, Hana; KAMINSKA, Katerina; HAJICEK, Josef
Patent: WO2011/57592 A1, 2011 ;
Location in patent: Page/Page column 16 ;
反应条件
tetrabutylammomium bromide; sodium hydrogencarbonate; potassium bromide in N,N-dimethyl-formamide T=40 - 55°C; 0.75 h; Inert atmosphere;
参考文献
Zhejiang Huahai Pharmaceutical co., Ltd.
Patent: US2012/142927 A1, 2012 ;
Location in patent: Page/Page column 3 ;
反应条件
1: 5,6,7,7a-tetrahydro-4H-thieno[3,2-c]pyridin-2-one p-toluenesulfonate With N-ethyl-N,N-diisopropylamine in acetonitrile T=20°C; 2: 3-cyclopropyl-1-(2-fluorophenyl)-3-oxopropyl methanesulfonate With tetraethylammonium bromide T=22 - 25°C;
参考文献
ZENTIVA, K.S.; STEPANKOVA, Hana; HAJICEK, Josef; DOUSA, Michal
Patent: WO2010/60389 A1, 2010 ;
Location in patent: Page/Page column 8-9 ;
反应条件
potassium hydrogencarbonate in acetonitrile T=10 - 15°C;
参考文献
Zhejiang Huahai Pharmaceutical co., Ltd.
Patent: US2012/142927 A1, 2012 ;
Location in patent: Page/Page column 3 ;
反应条件
1: 5,6,7,7a-tetrahydro-4H-thieno[3,2-c]pyridin-2-one p-toluenesulfonate; 3-cyclopropyl-1-(2-fluorophenyl)-3-oxopropyl methanesulfonate With N-ethyl-N,N-diisopropylamine in acetonitrile T=20°C; 1.5 h; 2: acetic anhydride With N-ethyl-N,N-diisopropylamine; 4-(N,N-dimethlyamino)pyridine in acetonitrile T=20°C; 2 h;
参考文献
WO2011/57592 A1, ;
Page/Page column 13; 14 ;
反应条件
1: α-cyclopropylcarbonyl-2-fluorobenzyl bromide; 5,6,7,7a-tetrahydro-4H-thieno[3,2-c]pyridin-2-one p-toluenesulfonate With N-ethyl-N,N-diisopropylamine in acetonitrile T=30°C; 0.5 h; 2: acetic anhydride With N-ethyl-N,N-diisopropylamine; 4-(N,N-dimethlyamino)pyridine in acetonitrile Product distribution / selectivity;
参考文献
WO2011/57592 A1, ;
Page/Page column 12 ;
