反应详情

2,4-Difluoro-N-[5-[4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1-(phenylsulfonyl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]benzenesulfonamide (81 mg, 0.106 mmol) was suspended in isopropanol (2 ml) and 2M sodium hydroxide (aq) (0.53 ml, 1.060 mmol) was added. The reaction mixture was stirred at RT for 2 h, the solvent removed and the residue dissolved in water (1 ml) and acidified to pH˜6 by the addition of 2M hydrogen chloride (aq). The resultant suspension was extracted with dichloromethane (3×2 ml), the organic layer separated (hydrophobic frit) and concentrated in vacuo to give a brown solid which dissolved in MeOH:DMSO (1 ml, 1:1, v/v) and purified by MDAP (method A). The appropriate fractions were concentrated in vacuo to give the title compound as a white solid (45 mg).

1. customthe solvent removed
2. dissolutionthe residue dissolved in water (1 ml)
3. additionacidified to pH˜6 by the addition of 2M hydrogen chloride (aq)
4. extractionThe resultant suspension was extracted with dichloromethane (3×2 ml)
5. customthe organic layer separated (hydrophobic frit)
6. concentrationconcentrated in vacuo
7. customto give a brown solid which
8. customDMSO (1 ml, 1:1, v/v) and purified by MDAP (method A)
9. concentrationThe appropriate fractions were concentrated in vacuo