Sodium Nitrite → HCID 59833795, compound

Participants

Reaction Steps

To a solution of N-[3-(7-amino-2-methylsulfanyl-pyrido[2,3-d]pyrimidin-6-yl)-4-chloro-phenyl]-3-trifluoromethyl-benzamide (1.0 g, 2.04 mmol) in TFA (10 mL) is slowly added NaNO2 (423 mg, 6.12 mmol) at 0° C. with stirring for 20 minutes. The solvents are evaporated, diluted with EtOAc and washed with saturated K2CO3, brine and water. The organic layer is dried, filtered and concentrated to give crude product, which is purified by flash silica gel column, eluting with CH2Cl2 (100%) gradient to CH2Cl2/MeOH(NH3, 2N)(93/7%), to give the title intermediate as a solid (0.644 g, 64.4%).

Provenance & Evidence