Cesium carbonate → (S)-tert-butyl 2-((7-(4-(piperazin-1-yl)phenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholine-4-carboxylate

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Reaction Steps

A solution of (S)-tert-butyl 2-((7-chloropyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholine-4-carboxylate (3.96 g, 10.43 mmol), 1-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)piperazine hydrochloride (4.4 g, 13.55 mmol), Pd(PPh3)4 (2.41 g, 2.09 mmol) and Cs2CO3 (10.19 g, 31.29 mmol) in 150 mL of dioxane and 3 mL of water, under N2, was stirred at 110° C. overnight. The volatiles were removed in vacuo, and the residues was purified by chromatography with MeOH/H2O (1:20-5:1) to give 4.747 g of title compound. MS (m/z)=506 (M+H)+.

Provenance & Evidence