Br[C:2]1[CH:3]=[C:4]([CH:6]=[C:7]([N:9]2[CH:13]=[CH:12][CH:11]=[N:10]2)[CH:8]=1)[NH2:5].[NH:14]1[CH2:21][CH2:20]C[C@H:15]1[C:16](O)=[O:17].[O-]P([O-])([O-])=O.[K+].[K+].[K+]>CS(C)=O.O1CCOCC1.[Cu]I>[O:17]1[CH2:16][CH2:15][N:14]([C:2]2[CH:3]=[C:4]([CH:6]=[C:7]([N:9]3[CH:13]=[CH:12][CH:11]=[N:10]3)[CH:8]=2)[NH2:5])[CH2:21][CH2:20]1The mixture of 3-bromo-5-(1H-pyrazol-1-yl)aniline (200 mg, 0.84 mmol), morphoine (0.22 mL, 2.52 mmol), proline (39 mg, 0.34 mmol), CuI (33 mg, 0.17 mmol) and K3PO4 (540 mg, 2.52 mmol) in 10 mL DMSO was stirred at 120° C. in a sealed tube for 4 days. It was diluted with dioxane, filtered through celite, concentrated in vacuo and subjected to reverse phase preparative HPLC to isolate 3-morpholino-5-(1H-pyrazol-1-yl)aniline (124 mg).
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