反应详情

According to Scheme 3 Step 4: A solution of 5-bromo-1-tosyl-6,7-dihydro-1H-indazol-4(5H)-one (0.90 mmol, 331 mg) and of 1-(6-methylpyridin-2-yl)thiourea (0.90 mmol, 150 mg) in EtOH (10 mL) and HCl (35%, 1 mL) was stirred at 80° C. for 5 hours. The reaction was quenched with the addition of a saturated solution of NaHCO3 at room temperature until pH=8. The aqueous phase was extracted with DCM. The organic phase was dried over Na2SO4 and concentrated. The crude residue was washed with Et2O and dried to yield N-(6-methylpyridin-2-yl)-5,6-dihydro-4H-thiazolo[4,5-e]indazol-2-amine (0.78 mmol, 220 mg, 87%) as a white solid.

1. customThe reaction was quenched with the addition of a saturated solution of NaHCO3 at room temperature until pH=8
2. extractionThe aqueous phase was extracted with DCM
3. dry with materialThe organic phase was dried over Na2SO4
4. concentrationconcentrated
5. washThe crude residue was washed with Et2O
6. customdried