反应详情

5-{2-Benzyloxy-4-[(E)-2-(2-benzyloxymethyl-2H-pyrazol-3-yl)-vinyl]-phenyl} 1,1-dioxo-1,2,5-thiadiazolidin-3-one (240 mg, 0.40 mmol) is dissolved in methanol (5 mL). 10% Pd/C is added periodically (7×50 mg) at intervals over 4 days. The mixture is stirred under an atmosphere of hydrogen at balloon pressure. The catalyst is removed by filtering the mixture through Celite and the filtrate is concentrated. The residue is chromatographed (reverse phase, 0-25% EtOH/water) to afford the title compound as a grey solid: 1H NMR (CD3OD) δ 7.46 (s, 1H), 7.31 (d, J=8.0 Hz, 1H), 6.75 (s, 1H), 6.71 (d, J=8.0 Hz, 1H) 6.10 (s, 1H) 4.29 (s, 2H), 2.89 (m, 4H); (M+1)+=323.

1. customThe catalyst is removed
2. filtrationby filtering the mixture through Celite
3. concentrationthe filtrate is concentrated
4. customThe residue is chromatographed (reverse phase, 0-25% EtOH/water)