反应详情

To a stirred solution of methyl 2-[(3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl]-4-[4-(piperidin-1-yl)pyrimidin-2-yl]-1,3-thiazole-5-carboxylate (Example 184, 35 mg. 0.06 mmol) in tetrahydrofuran (5 mL) was added a solution of lithium hydroxide (9.6 mg, 0.23 mmol) in water (1 mL). The reaction mixture was stirred at room temperature for 18 h. The reaction mixture was concentrated to dryness. The resulting residue was diluted with water (2 mL) and the aqueous layer was extracted with diethyl ether (2×10 mL). The aqueous layer was acidified to pH 4-5 with 2N HCl solution, solid obtained was filtered and dried to yield 2-[(3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl]-4-[4-(piperidin-1-yl)pyrimidin-2-yl]-1,3-thiazole-5-carboxylic acid 27 mg (79%).

1. concentrationThe reaction mixture was concentrated to dryness
2. additionThe resulting residue was diluted with water (2 mL)
3. extractionthe aqueous layer was extracted with diethyl ether (2×10 mL)
4. customobtained
5. filtrationwas filtered
6. customdried