Cesium carbonate → HCID 67107511, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of methyl 6-(benzenesulphonylmethyl)-2-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (Intermediate 59, 0.15 g), tri-tert-butyl-phosphinium tetrafluoroborate (0.01 g), cesium carbonate (0.34 g), tris-(dibenzylideneacetone)-dipalladium (0.016 g), and 4-bromoisothiazole (0.06 g) in dioxane (3.2 ml) and water (0.4 ml) was degassed and then heated in the microwave at 120° C. for 20 minutes. After cooling, the mixture was diluted with ether, dried (MgSO4) and filtered. The filtrate was evaporated to dryness and the residue was purified by chromatography on silica, eluting with a mixture of ethyl acetate and cyclohexane with a gradient of 0-60% to give crude methyl 6-(benzenesulphonylmethyl)-3-(isothiazol-4-yl)-2-methoxy-benzoate (0.044 g) as an oil. The material was used without further purification or characterisation.

Provenance & Evidence