反应详情

A solution of 1-(5-t-Butyl-2-{3-[5-(4-methoxy-benzyl)-(R)-3-methyl-1,1,4-trioxo-1λ6-[1,2,5]-thiadiazolidin-2-ylmethyl]-phenyl}-2H-pyrazol-3-yl)-3-naphthalen-1-yl-urea (20 mg, 0.030 mmol) in trifluoroacetic acid (2 mL) was stirred at 50° C. for 4 h. After the solvent was removed, the residue was purified by preparative-HPLC to afford 1-{5-t-butyl-2-[3-((R)-3-methyl-1,1,4-trioxo-1λ6-[1,2,5]thiadiazolidin-2-ylmethyl)-phenyl]-2H-pyrazol-3-yl}-3-naphthalen-1-yl-urea as a white power (6 mg). 1H NMR (DMSO-d6): 8.99 (s, 1H), 8.80 (s, 1 H), 8.00 (d, J=7.2 Hz, 1 H), 7.90 (d, J=7.2 Hz, 2 H), 7.60-7.64 (m, 2 H), 7.44-7.54 (m, 7 H), 6.41 (s, 1 H), 4.31-4.49 (dd, J=8.0 Hz, 2 H), 4.03 (q, J=7.6 Hz, 1 H), 1.27 (s, 9 H), 1.19 (d, J=8.0 Hz, 3 H). MS (ESI) m/z: 533 (M+H+).

1. customAfter the solvent was removed
2. customthe residue was purified by preparative-HPLC