Morpholine → (2S)-2-methyl-7-morpholin-4-yl-2-trifluoromethyl-2,3-dihydro-1H-imidazo[1,2-a]pyrimidin-5-one

Participants

Reaction Conditions

Reaction Steps

A mixture of 2.2 g of (2S)-7-chloro-2-methyl-2-(trifluoromethyl)-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one in 60 mL of morpholine is heated to 120° C. After one hour of heating and after monitoring with LC/MS, the reaction is completed. After cooling, the reaction mixture is concentrated under reduced pressure. On the obtained residue, 30 mL of cold water and 150 mL of ethyl acetate are added. The organic phase is then separated, dried on magnesium sulfate, filtered and then concentrated under reduced pressure in order to obtain 2.6 g of (2S)-2-methyl-7-(morpholin-4-yl)-2-(trifluoromethyl)-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one including the following characteristics:

Provenance & Evidence