3-氧代-3,4-二氢-2H-吡啶并[3,2-b][1,4]噻嗪-6-羧酸甲酯合成路线 （共 6 条）
反应条件
1: mercapto acetic acid ethylester With sodium hydride in N,N-dimethyl-formamide
T=0°C; 1 h;
2: methyl 6-amino-5-bromopyridine-2-carboxylate in N,N-dimethyl-formamide
T=20°C; 16 h;
参考文献
GLAXO GROUP LIMITED
Patent: WO2006/81178 A2, 2006 ;
Location in patent: Page/Page column 20-21 ;
反应条件
1: mercapto acetic acid ethylester With sodium hydride in N,N-dimethyl-formamide
T=0°C; 1 h;
2: methyl 6-amino-5-bromopyridine-2-carboxylate in N,N-dimethyl-formamide
T=20°C;
参考文献
Brooks, Gerald; Dabbs, Steven; Davies, David T.; Hennessy, Alan J.; Jones, Graham E.; Markwell, Roger E.; Miles, Timothy J.; Owston, Nathan A.; Pearson, Neil D.; Peng, Tony W.
Tetrahedron Letters, 2010 , vol. 51, # 38 p. 5035 - 5037
反应条件
1: 2-mercaptoacetic acid methyl ester With sodium hydride in N,N-dimethyl-formamide
1 h;
2: methyl 6-amino-5-bromopyridine-2-carboxylate in N,N-dimethyl-formamide
T=20°C; 12 h;
参考文献
MORPHOCHEM AKTIENGESELLSCHAFT FUeR KOMBINATORISCHE CHEMIE
Patent: WO2006/21448 A1, 2006 ;
Location in patent: Page/Page column 53 ;
反应条件
1: With sodium hydroxide; water in 1,4-dioxane
2 h;
2: With hydrogenchloride in 1,4-dioxane; water
pH=4;
参考文献
GLAXO GROUP LIMITED
Patent: WO2006/81178 A2, 2006 ;
Location in patent: Page/Page column 21 ;
反应条件
1: With lithium triethylborohydride in tetrahydrofuran
T=5 - 10°C; 1.16667 h;
2: With dihydrogen peroxide; acetic acid in tetrahydrofuran; methanol
T=10 - 37°C;
参考文献
ACTELION PHARMACEUTICALS LTD.
Patent: US2011/39836 A1, 2011 ;
Location in patent: Page/Page column 16-17 ;
反应条件
1.1: lithium triethylborohydride / tetrahydrofuran / 1.17 h / 5 - 10 °C
1.2: 1.17 h / 10 - 25 °C
2.1: manganese(IV) oxide / dichloromethane; tetrahydrofuran / 8 h
View Scheme
参考文献
ACTELION PHARMACEUTICALS LTD.
Patent: US2011/39836 A1, 2011 ;
