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0 °C

To a stirred solution of 7-chloro-1-(5-fluoro-3-methyl-2-(pyridin-2-yl)quinolin-4-yl)-2,3-dihydro-1H-pyrido[2,3-b][1,4]thiazine (30 mg, 0.071 mmol) in EtOAc (2.5 mL) was added disodium tungstate (2.08 mg, 7.09 μmol) and water (0.2 mL). The reaction was cooled at 0° C. and then H2O2 (36.2 μL, 0.355 mmol, 30%) was added. The reaction was allowed to warm to rt for 1 h. After this time more disodium tungstate (5 mg) was added followed by H2O2 (0.3 mL) and the reaction was stirred at rt overnight. After this time the reaction was diluted with EtOAc (50 mL) and treated with a saturated aqueous solution of NaHSO3 (10 mL). The separated organic layer was washed with brine (10 mL), dried over MgSO4, filtered and evaporated in vacuo to give 7-chloro-1-(5-fluoro-3-methyl-2-pyridin-2-ylquinolin-4-yl)-2,3-dihydro-1H-pyrido[2,3-b][1,4]thiazine 4,4-dioxide. Mass Spectrum (ESI) m/e=455.0 (M+1).

1. temperatureto warm to rt for 1 h
2. washThe separated organic layer was washed with brine (10 mL)
3. dry with materialdried over MgSO4
4. filtrationfiltered
5. customevaporated in vacuo