2-(甲基硫代)-5H-吡咯并[3,4-d]嘧啶-6(7H)-羧酸叔丁酯合成路线 （共 8 条）
反应条件
3-chloro-benzenecarboperoxoic acid in dichloromethane T=0°C; 5 h;
参考文献
MERCK and CO., INC.
Patent: WO2006/127530 A2, 2006 ;
Location in patent: Page/Page column 42 ;
WO 2006/127530 A2
反应条件
1: 2-methyl-2-thiopseudourea sulfate With sodium ethanolate in ethanol
0.833333 h; Cooling with ice;
2: 3-dimethylaminomethylene-4-oxo-pyrrolidine-1-carboxylic acid tert-butyl ester in ethanol
T=80°C; 16 h;
参考文献
ALLERGAN, INC.; Hull, III, Clarence E.; Malone, Thomas C.
Patent: US2013/237537 A1, 2013 ;
Location in patent: Paragraph 0294-0295 ;
反应条件
1: 2-methyl-2-thiopseudourea sulfate With sodium ethanolate in ethanol
T=0°C; 0.166667 h;
2: tert-butyl (3Z)-3-[(dimethylamino)methylene]-4-oxopyrrolidine-1 -carboxylate in ethanol
T=80°C; 2 h;
参考文献
MERCK and CO., INC.
Patent: WO2006/127530 A2, 2006 ;
Location in patent: Page/Page column 41-42 ;
WO 2006/127530 A2
反应条件
1: 3-Oxo-pyrrolidine-1-carboxylic acid tert-butyl ester With N,N-dimethyl-formamide dimethyl acetal
T=140°C; 1 h;
2: S-methylisothiourea sulfate With sodium ethanolate in ethanol
24 h; Heating / reflux;
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: EP1577302 A1, 2005 ;
Location in patent: Page/Page column 91 ;
反应条件
1: N,N-dimethyl-formamide dimethyl acetal; 3-Oxo-pyrrolidine-1-carboxylic acid tert-butyl ester T=20 - 140°C; 1 h;
2: S-methylisothiourea sulfate With sodium ethanolate in ethanol
T=20°C; 24 h; Heating / reflux;
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: EP1405852 A1, 2004 ;
Location in patent: Page 83 ;
EP 1405852 A1
反应条件
sodium ethanolate in ethanol; hexane
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: EP1270557 A1, 2003 ;
反应条件
1.1: 1,4-dioxane / 17 h / 100 °C
2.1: sodium ethanolate / ethanol / 0.83 h / |Cooling with ice
2.2: 16 h / 80 °C
View Scheme
参考文献
ALLERGAN, INC.; Hull, III, Clarence E.; Malone, Thomas C.
Patent: US2013/237538 A1, 2013 ;
反应条件
trifluoroacetic acid in dichloromethane
T=20°C; 3 h;
参考文献
ALLERGAN, INC.; Hull, III, Clarence E.; Malone, Thomas C.
Patent: US2013/237537 A1, 2013 ;
Location in patent: Paragraph 0296-0297 ;
