Morpholine → HCID 86598345, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of methanesulfonic acid (3R,7S,9aR)-3-benzyl-2-(3,5-bis(trifluoromethyl)benzoyl)-octahydropyrido[1,2-a]pyrazin-7-yl ester (1.97 g) and morpholine (0.44 mL) in acetonitrile (50 mL) was heated at 80° C. for 40 hours. After cooling to room temperature the mixture was concentrated in vacuo and the residue purified by flash-chromatography (SiO2, CH2Cl2/MeOH/NH4OH 980:18.75:1.25) to afford 3,5-bis(trifluoromethyl)phenyl-[(3R,7R,9aR)-3-benzyl-7-morpholin-4-yl-octahydropyrido[1,2-a]pyrazin-2-yl]-methanone (0.97 g, Rf 0.24 (CH2Cl2/MeOH/NH4OH 96:3.75:0.25)) (compound 29) and 3,5-bis(trifluoromethyl)phenyl-[(3R,7S,9aR)-3-benzyl-7-morpholin-4-yl-octahydropyrido[1,2-a]pyrazin-2-yl]-methanone (0.75 g, Rf 0.15 (CH2Cl2/MeOH/NH4OH 96:3.75:0.25)) (compound 30).

Provenance & Evidence