5-氟-1H-吲唑-3-羧酸乙酯合成路线 (共 3 条)
反应条件
sulfuric acid
T=20 - 80°C; 24 h; Inert atmosphere;
参考文献
Purdue Pharma L.P.; Kyle, Donald J.; Ni, Chiyou; Tafesse, Laykea; Yao, Jiangchao
Patent: US2013/296281 A1, 2013 ;
Location in patent: Paragraph 0580 ;
反应条件
1: 5-fluoro-1H-indazole-3-carboxylic acid With 1,1'-carbonyldiimidazole in tetrahydrofuran
2 h; Heating / reflux;
2: ethanol in tetrahydrofuran
5 h; Heating / reflux;
参考文献
Ackermann, Jean; Bleicher, Konrad; Ceccarelli, Simona M.; Chomienne, Odile; Mattei, Patrizio
Patent: US2008/103182 A1, 2008 ;
Location in patent: Page/Page column 18 ;
反应条件
1.1: sodium hydroxide / water / 0.5 h / 50 °C
1.2: 1 h / 0 °C
1.3: 18 h / 0 - 20 °C
2.1: sulfuric acid / 5 h / 100 °C
View Scheme
参考文献
Crocetti, Letizia; Schepetkin, Igor A.; Cilibrizzi, Agostino; Graziano, Alessia; Vergelli, Claudia; Giomi, Donatella; Khlebnikov, Andrei I.; Quinn, Mark T.; Giovannoni, Maria Paola
Journal of Medicinal Chemistry, 2013 , vol. 56, # 15 p. 6259 - 6272