[CH3:1][C:2]1[NH:6][C:5]2[C:7](=[O:10])[CH2:8][CH2:9][C:4]=2[C:3]=1[C:11]([OH:13])=O.[CH:14]1[CH:15]=[CH:16][C:17]2N(O)N=N[C:18]=2[CH:19]=1.C(Cl)CCl.[NH2:28][C:29]1C=CC=CC=1>CN(C=O)C.C([O-])([O-])=O.[Na+].[Na+].O>[CH2:29]([NH:28][C:11]([C:3]1[C:4]2[CH2:9][CH2:8][C:7](=[O:10])[C:5]=2[NH:6][C:2]=1[CH3:1])=[O:13])[C:18]1[CH:17]=[CH:16][CH:15]=[CH:14][CH:19]=1A mixture of 2-methyl-6-oxo-1,4,5,6-tetrahydro-cyclopenta[b]pyrrole-3-carboxylic acid (Example B, 268.5 mg, 1.5 mmol), HOBt (202.5 mg, 1.5 mmol) and EDC (573.5 mg, 3 mmol) in dry DMF (5 mL) was stirred at room temperature for 20 min. Then aniline (3.0 mmol) was added to the mixture and stirring was continued for 24 hours. The reaction was diluted with sat. Na2CO3 and water, the solid was collected by vacuum filtration, washed with sat. Na2CO3 and water in turn, dried to give 315 mg of the titled compound as a white solid.
Wird geladen…