[CH2:1]1[C:3]2([CH2:7][CH2:6][N:5]([C:8]3[CH:9]=[C:10]([NH2:16])[C:11]([NH2:15])=[CH:12][C:13]=3[Cl:14])[CH2:4]2)[CH2:2]1.[C:17]([O:21][C:22](=[O:35])[NH:23][CH2:24][C:25]1[CH:30]=[CH:29][C:28]([Cl:31])=[C:27]([N:32]=[C:33]=S)[CH:26]=1)([CH3:20])([CH3:19])[CH3:18]>CN(C=O)C>[C:17]([O:21][C:22](=[O:35])[NH:23][CH2:24][C:25]1[CH:30]=[CH:29][C:28]([Cl:31])=[C:27]([NH:32][C:33]2[NH:16][C:10]3[CH:9]=[C:8]([N:5]4[CH2:6][CH2:7][C:3]5([CH2:1][CH2:2]5)[CH2:4]4)[C:13]([Cl:14])=[CH:12][C:11]=3[N:15]=2)[CH:26]=1)([CH3:20])([CH3:19])[CH3:18]TEA (130 μL, 0.9 mmol) followed by 4-(5-aza-spiro[2.4]hept-5-yl)-5-chloro-benzene-1,2-diamine (80 mg) were added to (4-chloro-3-isothiocyanato-benzyl)-carbamic acid tert-butyl ester (example 1, step (c), 69 mg, 0.2 mmol) in DMF (3 mL). The reaction mixture was stirred at rt overnight, then concentrated and purified by chromatography to give the sub-title compound.
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