Cesium carbonate → (S)-2,2-difluoro-1-(2-((7-(4-(piperazin-1-yl)phenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholino)ethanone

Participants

Reaction Steps

A solution of (S)-1-(2-((7-chloropyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholino)-2,2-difluoroethanone (70 mg, 0.19 mmol), 1-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)piperazine hydrochloride (96 mg, 0.29 mmol), Pd(PPh3)4 (45 mg, 0.04 mmol) and Cs2CO3 (191 mg, 0.59 mmol) in 8 mL of dioxane and 0.1 mL of water, under N2, was stirred at 110° C. overnight. The volatiles were removed in vacuo, and the residue was purified by chromatography with MeOH/H2O (1:10˜8:1) to give 100 mg of title compound.

Provenance & Evidence