[SH:1][CH:2](O)C.[Cl:5][C:6]1[C:7]([NH:26][C:27](=[O:35])[CH2:28][CH:29]2[CH2:34][CH2:33][CH2:32][CH2:31][CH2:30]2)=[C:8]2[C:13](=[CH:14][CH:15]=1)[N:12]=[C:11]([N:16]1[CH2:20][CH2:19][C@H:18](OS(C)(=O)=O)[CH2:17]1)[CH:10]=[CH:9]2.[C:36](=[O:39])([O-])[O-].[K+].[K+]>CN(C)C=O>[Cl:5][C:6]1[C:7]([NH:26][C:27](=[O:35])[CH2:28][CH:29]2[CH2:34][CH2:33][CH2:32][CH2:31][CH2:30]2)=[C:8]2[C:13](=[CH:14][CH:15]=1)[N:12]=[C:11]([N:16]1[CH2:20][CH2:19][C@H:18]([S:1][CH2:2][CH2:36][OH:39])[CH2:17]1)[CH:10]=[CH:9]2Mercaptoethanol (0.073 mL) was added to N-[6-chloro-2-[(3S)-3-[(methylsulfonyl)oxy]-1-pyrrolidinyl]-5-quinolinyl]-cyclohexaneacetamide (Example 33(a)) (0.1 g) and potassium carbonate (0.24 g) in dry N,N-dimethylformamide. The reaction mixture was heated at 60° C. in a microwave for 2 hours and then partitioned between water and ethyl acetate. The combined organics were washed with brine, dried and concentrated. Purification (SiO2, methanol:dichloromethane 3:97 as eluant) gave the sub-titled compound as a solid (0.05 g).
Wird geladen…