N-methyl-2-pyrrolidone → HCID 69003486, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 5,6-dichloro-4-fluoro-3-(2-fluorophenylamino)-pyridine-2-carboxylic acid methyl ester (1.00 equivalent) (prepared in Example 8), dppf (0.02 equivalents), Pd2dba3 (0.01 equivalents), and Zn(CN)2 (0.60 equivalents) in NMP is stirred at 120° C. in a sealed tube. After stirring for 20 hours, the reaction mixture is cooled to room temperature and quenched with a 4:1:4 (volume) mixture solution of saturated aqueous NH4Cl-conc NH4OH-water. The mixture is extracted with EtOAc. The organic layer is washed with saturated aqueous NH4Cl/conc. NH4OH/water, and brine. The organic layer is dried over MgSO4, filtered, and concentrated in vacuo to give the crude material that is purified by flash column chromatography to afford the desired product.

Provenance & Evidence