反应详情

Trifluoroacetic acid (1.73 mL, 22.20 mmol, 15.0 eq) is added at 0° C. to a stirred solution of 4-[(3-oxo-3,4-dihydro-2H-benzo[1,4]thiazine-6-carbonyl)-amino]-piperidine-1-carboxylic acid tert-butyl ester (610 mg, 1.48 mmol, 1.0 eq) in dichloromethane (20 mL). After 2 hours stirring at room temperature, the reaction mixture is extracted with dichloromethane (3×20 mL) and water (20 mL) and the pH is adjusted to 12 by the addition of a 1N sodium hydroxide aqueous solution. The combined organic layers are dried over sodium sulfate, filtered and concentrated to afford 3-oxo-3,4-dihydro-2H-benzo[1,4]thiazine-6-carboxylic acid piperidin-4-ylamide as a light brown solid (244 mg, 51% yield).

1. extractionthe reaction mixture is extracted with dichloromethane (3×20 mL) and water (20 mL)
2. additionthe pH is adjusted to 12 by the addition of a 1N sodium hydroxide aqueous solution
3. dry with materialThe combined organic layers are dried over sodium sulfate
4. filtrationfiltered
5. concentrationconcentrated