Cesium carbonate → 3-{4-[2-(2-Cyclopropylmethoxy-pyridin-3-yl)-5,6-difluoro-benzoimidazol-1-ylmethyl]-phenyl}-propionic acid methyl ester

Participants

Reaction Steps

To a stirred solution of 3-{4-[5,6-difluoro-2-(2-hydroxy-pyridin-3-yl)-benzoimidazol-1-ylmethyl]-phenyl}-propionic acid methyl ester (72 mg, 0.17 mmol) in acetone (10 ml) was added cesium carbonate (85 mg, 0.26 mmol) followed by bromomethyl-cyclopropane (26 mg, 0.19 mmol; CAS Reg. No. 7051-34-5) and the reaction was refluxed for 2 h. The reaction mixture was filtered and the filtrate removed under reduced pressure. The residue was purified by column chromatography using silica gel (50-60% ethyl acetate/n-hexane) to afford the desired product as a brown solid (67%). MS (Turbo Spray): m/z=478.5 (M+H).

Provenance & Evidence