Cesium carbonate → HCID 66906112, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-hydroxypiperidine (2.65 g, 25.4 mmol), methyl 4-bromo-3-methylbenzoate (5.00 g, 21.8 mmol), (R)-(+)-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (1.37 g, 2.17 mmol), palladium acetate (0.247 g, 1.10 mmol), cesium carbonate (21.5 g, 65.3 mmol) in 1,4-dioxane (100 mL) is heated in a 350 mL pressure vessel for 18 h at 80° C. under nitrogen and then at 120° C. for 4 h. The mixture is filtered and concentrated under reduced pressure. The residue is purified on silica (120 g) using a gradient of 0 to 90% ethyl acetate in heptane to provide the title compound (2.4 g, 44%). LC-ES/MS m/z 250.2 (M+1)

Provenance & Evidence