Cesium carbonate → Methyl (+)-{4-[4-(4-Amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohex-3-en-1-yl}acetate

Participants

Reaction Steps

A stirred solution of 4-amino-6-(4-iodophenyl)-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5(6H)-one (40 mg, 0.10 mmol), methyl[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)cyclohex-3-en-1-yl]acetate (38 mg, 0.14 mmol), cesium carbonate (42 mg, 0.28 mmol) and palladium tetrakis(triphenyl-phosphine) (6 mg, 0.005 mmol) in 1,2-dimethoxyethane (1.0 mL) was heated at 100° C. for 18 hours. The reaction mixture was cooled, concentrated and chromatographed to afford a white solid, 19 mg. IC50 84.3 nM.

Provenance & Evidence