Cesium carbonate → 3-Benzyloxy-1-(toluene-4-sulfonylmethyl)-1H-pyridin-2-one

Participants

Reaction Conditions

Reaction Steps

To a suspension of 3-benzyloxy-1H-pyridin-2-one (0.22 g, 1.1 mmol) from step A and Cs2CO3 (0.72 g, 2.2 mmol) in dry DMF (5 mL) was added 1-chloromethanesulfonyl-4-methyl-benzene (0.31 g, 1.54 mmol). The reaction mixture was heated at 95° C. overnight and then additional 1-chloromethanesulfonyl-4-methyl-benzene (0.22 g, 1.1 mmol) was added. The reaction mixture was stirred for another 18 h. After the usual work-up, the crude material was purified by chromatography (silica gel, 40% EtOAc/hexanes) to give the product. MS (EI) 370 (M+H)+.

Provenance & Evidence