反应详情

N-{6-[5-{[(2,4-Difluorophenyl)sulfonyl]amino}-6-(methyloxy)-3-pyridinyl]-1-[(4-methylphenyl)sulfonyl]-1H-indazol-4-yl}-2-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-thiazole-4-carboxamide (105 mg) was dissolved in IPA (1 mL) and 2M NaOH (aq) (1 mL) and stirred at room temperature overnight. The IPA was evaporated and the remaining aqueous phase was diluted with water (2 ml), then acidified to ca. pH 4 using 2M HCl (aq) to give a precipitate that was extracted into DCM, passed through a hydrophobic frit, then evaporated to dryness. The residue was purified by ISCO companion 12 g silica cartridge using a 0-6% methanol in DCM gradient over 16 mins at 30 ml/min. Product containing fractions were combined, evaporated to dryness then further dried on a vacuum line to give title compound, (53 mg).

1. customThe IPA was evaporated
2. additionthe remaining aqueous phase was diluted with water (2 ml)
3. customto give a precipitate that
4. extractionwas extracted into DCM
5. customevaporated to dryness
6. customThe residue was purified by ISCO companion 12 g silica cartridge
7. customover 16 mins
8. additionProduct containing fractions
9. customevaporated to dryness
10. customthen further dried on a vacuum line