Potassium Phosphate, Tribasic → 2-(3-Hydroxyphenyl)-8-oxo-9-(piperidin-4-YL)-8,9-dihydro-7H-purine-6-carboxamide

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Reaction Steps

Ethyl 5-amino-6-(1-(tert-butoxycarbonyl)piperidin-4-ylamino)-2-(3-hydroxyphenyl)pyrimidine-4-carboxylate. Ethyl 5-amino-6-(1-(tert-butoxycarbonyl)piperidin-4-ylamino)-2-chloropyrimidine-4-carboxylate. (0.400 g, 1.00 mmol) 3-hydroxyphenyl boronic acid (0.207 g, 1.5 mmol), palladium(II)acetate (0.034 g, 0.15 mmol), potassium phosphate (0.430 g, 2.0 mmol) and dicyclohexyl(2,6-dimethoxyphenyl)phosphine (0.062 g, 0.15 mmol) were combined in tetrahydrofuran (6 mL) and water (0.6 ml) and reacted in the microwave at 120° C. for 30 min. The reaction was monitored via thin layer chromatography for consumption of starting materials. The solution was filtered and concentrated and the residue purified via Biotage chromatography (0-60% EtOAc in hexanes) to afford the title compound (0.120 g, 40%). MS (ESI) m/z 458.5 [M+1]+.

Provenance & Evidence