反应详情

A solution of methyl 2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-4-fluoro-5-[(hydroxyimino)(1,3-thiazol-2-yl)methyl]-3-methylbenzoic acid (Intermediate 195, 0.31 g, 0.8 mmol), K2CO3 (0.4 g, 2.3 mmol) and potassium iodide (0.03 g, 0.2 mmol) in DMF (10 mL) was heated at 130° C. for 12 hours. Solvents were removed under vacuum and the residue was treated with 1.5N hydrochloric acid and extracted with ethyl acetate, which was dried over sodium sulfate. Removal of solvent by vacuum afforded product. Yield: 0.18 g (62%).

1. customSolvents were removed under vacuum
2. additionthe residue was treated with 1.5N hydrochloric acid
3. extractionextracted with ethyl acetate, which
4. dry with materialwas dried over sodium sulfate
5. customRemoval of solvent by vacuum
6. customafforded product