Sodium Carbonate → HCID 70979619, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of ethyl 5-(2-aminopyrimidin-4-yl)-2-bromo-1H-pyrrole-3-carboxylate (prepared according to WO2007/110344, 2.0 g, 6.43 mmol) dissolved in EtOH (20 mL) and toluene (20 mL), LiCl (408 mg, 9.64 mmol), 1 M aq Na2CO3 (17 mmol), 2-chloro-5-trifluoromethylphenylboronic acid (1.875 g, 8.35 mmol) and (Ph3P)2PdCl2 (470 mg, 0.67 mmol) were added and the reaction mixture was heated at 100° C. for 5 h. After cooling to room temperature, the precipitate was filtered and the filtrate was evaporated under reduced pressure, dissolved in DCM and washed with water. The organic layer was then dried over sodium sulfate and concentrated. The crude material was chromatographed on silica gel (DCM/EtOAc 50/50) to afford the title compound (2.16 g, 82%).

Provenance & Evidence