反应详情

温度

90 °C

To a stirred suspension of ethyl 1-[2-(dimethylamino)ethyl]-6-{6-[(ethylcarbamoyl)amino]-4-[4-(trifluoromethyl)-1,3-thiazol-2-yl]pyridin-3-yl}-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylate (Example 15, 100 mg, 0.16 mmol) in ethanol (10 mL) 10% potassium hydroxide (0.3 mL) was added. The reaction mixture was heated to 90° C. for 1 h. After completion of the reaction, the reaction mixture was cooled to room temperature then concentrated under reduced pressure to a residue. The residue was diluted with water and acidified with 2N HCl to pH 2-3 to obtain a solid which was filtered, washed with water and dried to afford 50 mg of crude product. This was purified by preparative HPLC to give 15 mg (15%) of 1-[2-(dimethylamino)ethyl]-6-{6-[(ethylcarbamoyl)amino]-4-[4-(trifluoromethyl)-1,3-thiazol-2-yl]pyridin-3-yl}-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid.

1. additionwas added
2. customAfter completion of the reaction
3. temperaturethe reaction mixture was cooled to room temperature
4. concentrationthen concentrated under reduced pressure to a residue
5. additionThe residue was diluted with water
6. customto obtain a solid which
7. filtrationwas filtered
8. washwashed with water
9. customdried
10. customto afford 50 mg of crude product
11. customThis was purified by preparative HPLC