反应详情

Lithium hydroxide monohydrate (6 mg, 0.14 mmol) in water (1 mL) was added to a solution of methyl 5-[(3-{[(1S)-1-(hydroxymethyl)propyl]oxy}-5-{[(1-methyl-1H-pyrazol-3-yl)amino]carbonyl}phenyl)oxy]pyrazine-2-carboxylate (25 mg, 0.06 mmol) in THF (1 mL). The mixture was allowed to stir at RT for 16 hours. The THF was removed in vacuo and the resulting solution was partitioned between water (10 mL) and ethyl acetate (25 mL), the ethyl acetate layer was washed with brine (10 mL) and dried (MgSO4). The aqueous layer was then adjusted to pH 7 by addition of 1M hydrochloric acid and extracted with ethyl acetate (25 mL). The ethyl acetate layer was washed with brine (10 mL) and dried (MgSO4). The ethyl acetate extracts were combined and evaporated to give the required product (12 mg). m/z 428.44 (M+H)+

1. customThe THF was removed in vacuo
2. customthe resulting solution was partitioned between water (10 mL) and ethyl acetate (25 mL)
3. washthe ethyl acetate layer was washed with brine (10 mL)
4. dry with materialdried (MgSO4)
5. additionThe aqueous layer was then adjusted to pH 7 by addition of 1M hydrochloric acid
6. extractionextracted with ethyl acetate (25 mL)
7. washThe ethyl acetate layer was washed with brine (10 mL)
8. dry with materialdried (MgSO4)
9. customevaporated