Methylamine → HCID 11855959, compound

Participants

Reaction Conditions

Reaction Steps

Carbonyldiimidazole (180 mg, 1.11 mmol) was added to a stirred suspension of the acid, 4-[2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-nicotinic acid (240 mg, 0.56 mmol) in dry DMF (15 ml). The reaction was heated to 60° C. for 2 hours under nitrogen. The reaction was cooled to room temperature and MeNH2 (2M in THF, 5 equivalents) was added and the reaction stirred for 18 hours. The reaction mixture was partitioned between CHCl3 (50 mL) and water (50 mL). The organic layer was further washed with water (3×50 mL). The product precipitated out of the CHCl3 solution and was filter to give compound 4-[2-(5-Chloro-2-methylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide (47 mg, 19% yield).

Provenance & Evidence