反应详情

To a stirred solution of 7-(3-{1-[(1-tert-butoxycarbonyl-piperidin-4-yl)-methyl-amino]-cyclopropyl}-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid in dichloroethane (2.0 mL) was added trifluoroacetic acid (1.0 mL, ˜13 mmol) at 0° C. during a period of 5-6 minutes. The resulting solution was stirred at room temperature for one hour. The solvent was removed to yield yellow oil, which was partitioned between CH2Cl2 and sat. aq NaHCO3. The separated aqueous phase was extracted with CH2Cl2. The combined organic layer was with brine, dried over sodium sulfate and concentrated in vacuo. Title compound was achieved as a yellow solid (85 mg, 100%). ESI MS m/z 499.4 (M+H+).

1. customThe solvent was removed
2. customto yield yellow oil, which
3. customwas partitioned between CH2Cl2 and sat. aq NaHCO3
4. extractionThe separated aqueous phase was extracted with CH2Cl2
5. dry with materialdried over sodium sulfate
6. concentrationconcentrated in vacuo