Potassium Phosphate, Tribasic → HCID 178513786, compound

Participants

Reaction Steps

Ethyl 5-amino-6-(trans-4-(tert-butoxycarbonylamino)cyclohexylamino)-2-(3-hydroxyphenyl)pyrimidine-4-carboxylate. Ethyl 5-amino-6-(trans-4-(tert-butoxycarbonylamino)cyclohexylamino)-2-chloropyrimidine-4-carboxylate. (0.500 g, 1.21 mmol), 3-hydroxyphenylboronic acid (0.249 g, 1.81 mmol), dicyclohexyl(2′,6′-dimethoxybiphenyl-2-yl)phosphine (0.075 g, 0.182 mmol), palladium acetate (0.041 g, 0.182 mmol) and potassium phosphate (0.52 g, 2.42 mmol) were combined in tetrahydrofuran (7 mL) and water (0.6 mL) and heated to 120° C. in a Biotage Emrys Optimizer microwave reactor for thirty min. The reaction solution was filtered and concentrated. The residue purified via Biotage chromatography (0 to 60% ethyl acetate in hexanes) to afford the title compound (0.150 g, 26%). MS (ESI) m/z 472[M+1]+.

Provenance & Evidence