Cesium carbonate → HCID 68905917, compound

Participants

Reaction Conditions

Reaction Steps

A microwave tube is charged with [4-(6-bromobenzo[b]thiophen-2-yl)-5-chloropyrimidin-2-yl]-[3-(4-methylpiperazin-1-yl)-propyl]-amine (0.045 g, 0.094 mmol), 1.5 equivalent of 2-pyrrolidinone (0.012 g, 0.14 mmol), 4 mol % of palladium acetate (0.010 g, 0.0040 mmol), 8 mol % of Xantphos (0.050 g, 0.0080 mmol), 1.5 equivalent of cesium carbonate (0.049 g, 0.15 mmol) and acetonitrile (2 mL). The reaction is sealed and heated under microwave condition at 150° C. for 15 minutes, cooled down, filtered and then evaporated to furnish a red oil. The crude material is subjected to reverse phase purification, eluting with 20-95% CH3CN/0.01 N NH4HCO3 in water, using a C18 Xterra column, to provide the title compound as a pale yellow solid (0.012 g, 23% yield). ES+(m/z) 485 (35Cl) and 487 (37Cl) [M+H].

Provenance & Evidence