反应详情

温度

50 °C

A solution of 300 mg (RS)-(4-cyano-phenylamino)-[5-ethoxy-2-fluoro-3-(piperidin-4-yloxy)-phenyl]-acetic acid ethyl ester described in example 11.2 in 10 ml THF was treated with 0.19 ml triethylamine, 0.82 ml 2-bromoethanol and 25 mg tetrabutylammonium iodide. The reaction mixture was heated to 50° C. for 6 hrs, then evaporated. The residue was taken up in water and extracted with EtOAc. The crude product was purified by chromatography on silica with dichloromethane/MeOH 9:1 to give 175 mg (RS)-(4-cyano-phenylamino)-{5-ethoxy-2-fluoro-3-[1-(2-hydroxy-ethyl)-piperidin-4-yloxy]-phenyl}acetic acid ethyl ester. MS: 486.4 ([M+H]+).

1. customevaporated
2. extractionextracted with EtOAc
3. customThe crude product was purified by chromatography on silica with dichloromethane/MeOH 9:1