Cesium carbonate → (8S)-9-(4-fluorobenzyl)-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one

Participants

Reaction Conditions

Reaction Steps

0.536 g of caesium carbonate and 0.44 ml of 1-(bromomethyl)-4-fluorobenzene are added, under an argon atmosphere, to a solution of 300 mg of (S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydro-pyrimido[1,2-a]pyrimidin-4-one (Example 1e) in 3 ml of acetonitrile. The resulting mixture is then heated at 80° C. for 2 hours. The reaction mixture is then evaporated under reduced pressure and the residue obtained is then purified by silica chromatography (eluent: CH2Cl2/MeOH 98/02) so as to give 61 mg of (8S)-9-(4-fluorobenzyl)-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, in the form of a white solid, the characteristics of which are the following:

Provenance & Evidence