反应详情

To a suspension of tert-butyl 5-(2-(3-((R)-1-(2,2,2-trifluoroacetyl)-pyrrolidine-2-carboxamido)phenyl)quinazolin-4-ylamino)-1H-indazole-1-carboxylate (100 mg, 0.15 mmol) in MeOH (5.7 mL) and H2O (345 mL) was added K2CO3 (108 mg, 0.78 mmol). Reaction mixture was refluxed for 2 h. Cooled to RT temperature and concentrated in vacuo. The residue was dissolved in EtOAc and extracted with H2O (3×). Dried the organic layer under Na2SO4 and concentrated in vacuo. The aqueous layer was basicified with 1 N NaOH, extracted with CHCl3 (3×), dried under Na2SO4 and concentrated in vacuo. The two organic layers were combined to afford tert-butyl 5-(2-(3-((R)-pyrrolidine-2-carboxamido)phenyl)quinazolin-4-ylamino)-1H-indazole-1-carboxylate. (65 mg, 79%).

1. customReaction mixture
2. temperaturewas refluxed for 2 h
3. concentrationconcentrated in vacuo
4. dissolutionThe residue was dissolved in EtOAc
5. extractionextracted with H2O (3×)
6. customDried the organic layer under Na2SO4
7. concentrationconcentrated in vacuo
8. extractionextracted with CHCl3 (3×)
9. customdried under Na2SO4
10. concentrationconcentrated in vacuo