反应详情

A suspension of 4-{3-[(1S)-2-hydroxy-1-methylethoxy]-5-[(1H-pyrazol-3-ylamino)carbonyl]phenoxy}benzoic acid (130 mg, 0.327 mmol), HATU (156 mg, 0.41 mmol), azetidine hydrochloride (38 mg, 0.41 mmol) and DIPEA (0.143 mL; 0.82 mmol) in DMF (2 mL) was stirred at ambient temperature for 16 hours. Water was added to the reaction mixture and it was extracted into ethyl acetate (3×30 mL). The organic phases were combined, washed with brine solution and dried (MgSO4). The filtrate was concentrated in vacuo and the residue chromatographed, eluting with 0-50% methanol in DCM, to give a clear oil which gave a foam under high vacuum (65 mg, 46%).

1. extractionwas extracted into ethyl acetate (3×30 mL)
2. washwashed with brine solution
3. dry with materialdried (MgSO4)
4. concentrationThe filtrate was concentrated in vacuo
5. customthe residue chromatographed
6. washeluting with 0-50% methanol in DCM
7. customto give a clear oil which
8. customgave a foam under high vacuum (65 mg, 46%)