Dimethylformamide → 2-Chloro-6-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-N-(2-morpholin-4-ylethyl)pyrimidine-4-carboxamide

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Reaction Steps

A solution of methyl 2-chloro-6-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)pyrimidine-4-carboxylate (Example 6: 380 mg, 0.85 mmol), 2-morpholin-4-ylethanamine (222 mg, 1.70 mmol) and TEA (0.12 ml, 0.85 mmol) in DMF (3 ml) were stirred at 60° C. under nitrogen for 18 hours. The mixture was cooled to room temperature and diluted with EtOAc (75 ml) and water (10 ml). The organic layer was separated, dried over Na2SO4, filtered and concentrated under vacuum. Purification by reversed-phase HPLC (water/acetonitrile gradient, 5-95%) provided 110 mg of the title compound.

Provenance & Evidence