Cesium carbonate → 3-(3,4-dimethoxybenzyl)-6-(2-fluoroethoxy)-1-(tetrahydro-2H-pyran-4-yl)-quinazoline-2,4(1H,3H)-dione

Participants

Reaction Steps

A mixture of 0.2 g of 3-(3,4-dimethoxybenzyl)-6-hydroxy-1-(tetrahydro-2H-pyran-4-yl)-quinazoline-2,4(1H,3H)-dione and 0.32 g of Cs2CO3 in 10 ml of DMF is irradiated in a microwave field for 1 minute at 100° C. 0.169 g of fluoroethanol are then added and the mixture is irradiated in a microwave field for 5 minutes at 140° C. The reaction medium is evaporated under reduced pressure. The residue is taken up in EtOAc and washed with water and then with saturated NaCl solution. The resulting solution is dried over Na2SO4, filtered and evaporated under reduced pressure. The residue is chromatographed on silica gel, eluting with a DCM/EtOAc mixture from (80/20, v/v) to give 0.212 g of the expected product.

Provenance & Evidence