Cesium carbonate → HCID 18336822, compound

Participants

Reaction Conditions

Reaction Steps

To a stirred solution of 2,6-dichloro-9-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)-9H-purine 2(1.0 g) in toluene (25 ml) was added palladium acetate (50 mg), 4-chloro-2-fluoroaniline (0.5 ml) and bis[2-(diphenylphosphino)phenyl] ether 3(120 mg) and the reaction stirred at 20° C. for 15 min. Caesium carbonate (872 mg) was added and the mixture heated at 90° C. for 16 hours. The reaction mixture was cooled to 20° C. and partitioned between ethyl acetate (100 ml) and water (100 ml). The organic layer was washed with brine (100 ml), dried with magnesium sulphate and the solvent removed in vacuo. Purification by flash chromatography on silica gel, eluting with ethyl acetate:cyclohexane (1:1) gave the title compound (400 mg).

Provenance & Evidence