N-(2-(二乙基氨基)乙基)-5-甲酰基-2,4-二甲基-1H-吡咯-3-甲酰胺合成路线 (共 19 条)
反应条件
sodium hydroxide; triethylamine in N-methyl-acetamide; methanol; dichloromethane; water; ethyl acetate; toluene
参考文献
Sugen. Inc.
Patent: US2003/100555 A1, 2003 ;
US 20030100555 A1
反应条件
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride in N,N-dimethyl-formamide T=5 - 20°C;
参考文献
Zou, Hongbin; Zhang, Liang; Ouyang, Jingfeng; Giulianotti, Marc A.; Yu, Yongping
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 12 p. 5970 - 5977
反应条件
1: tetrahydrofuran / 45 °C 2: imidazole / carbon dioxide / tetrahydrofuran / 45 °C 3: 100 percent / H2O View Scheme
参考文献
Journal of Organic Chemistry, , vol. 69, # 7 p. 2565 - 2568
反应条件
1: imidazole / carbon dioxide / tetrahydrofuran / 45 °C 2: 100 percent / H2O View Scheme
参考文献
Journal of Organic Chemistry, , vol. 69, # 7 p. 2565 - 2568
反应条件
1: 90 percent / aq. KOH / methanol / 3 h / Heating 2: 50 percent / EDC; HOBt; Et3N / dimethylformamide / 20 °C View Scheme
参考文献
Bioorganic and medicinal chemistry letters, , vol. 12, # 16 p. 2153 - 2157
反应条件
1: 81 percent / TFA / -5 - 20 °C 2: 90 percent / aq. KOH / methanol / 3 h / Heating 3: 50 percent / EDC; HOBt; Et3N / dimethylformamide / 20 °C View Scheme
参考文献
Bioorganic and medicinal chemistry letters, , vol. 12, # 16 p. 2153 - 2157
参考文献
Sugen, Inc.
Patent: US2003/69297 A1, 2003 ;
反应条件
1.1: trichlorophosphate / 2 - 3 h / 0 - 50 °C 1.2: 25 - 30 °C / pH 12 - 13 2.1: potassium hydroxide; water / methanol / 4 - 6 h / 60 - 70 °C 3.1: dicyclohexyl-carbodiimide; benzotriazol-1-ol / tetrahydrofuran / 0.5 h 3.2: 16 h / 25 - 30 °C View Scheme
反应条件
pyrrolidine in ethanol 5 h; Reflux;
参考文献
LEK PHARMACEUTICALS D.D.; SELIC, Lovro
Patent: WO2010/49449 A2, 2010 ;
Location in patent: Page/Page column 16; 17 ;
反应条件
1: 5-fluoro-1-(trimethylsilyl)-2-(trimethylsilyloxy)-1H-indole; 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylamino-ethyl)-amide With trimethylsilyl trifluoromethanesulfonate in acetonitrile 13 h; Reflux; 2: (-)-(S)-hydroxybutanedioic acid in methanol; acetonitrile T=20°C; 22 h;
参考文献
SCINOPHARM (KUNSHAN) BIOCHEMICAL TECHNOLOGY CO., LTD.; HENSCHKE, Julian, P.; CHEN, Yung-Fa
Patent: WO2012/58780 A1, 2012 ;
Location in patent: Page/Page column 30 ;