Cesium carbonate → tert-butyl 4-[6-(4-fluoro-2-methoxyphenyl)-2,4-dioxo-1,4-dihydrothieno[3,2-d]pyrimidin-3(2H)-yl]piperidine-1-carboxylate

Participants

Reaction Steps

Tert-butyl 4-(6-bromo-2,4-dioxo-1,4-dihydrothieno[3,2-d]pyrimidin-3(2H)-yl)piperidine-1-carboxylate (3.00 g, compound B53), (4-fluoro-2-methoxyphenyl)boronic acid (1.30 g) and dichlorobis(tricyclohexylphosphine)palladium (257 mg) are reacted in the presence of aqueous cesium carbonate solution (5.23 ml, 2.0 M) in DME (12 ml) according to the procedure described in example B55. The reaction mixture is poured into ice-cold water and the mixture is extracted with DCM. The organic layer is washed with saturated aqueous sodium chloride solution and filtered using a phase separator. All volatile materials are removed in vacuo to yield the title compound as a solid.

Provenance & Evidence