Morpholine → (S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-one

Participants

Reaction Steps

A mixture of 1 g of (8S)-2-chloro-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one and of 15 mL of morpholine is heated to 80° C. After one hour and a half 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, 10 mL of cold water and 100 mL of ethyl acetate are added. The resulting organic phase is separated and then dried on magnesium sulfate, filtered and concentrated under reduced pressure in order to obtain 1.2 g of (8S)-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one including the following characteristics:

Provenance & Evidence