Morpholine → 7-(5-morpholin-4-ylmethyl-2-oxooxazolidin-3-yl)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one

Participants

Reaction Steps

The 2-oxo-3-[1-oxo-3-(2-trifluoromethylphenyl)-1,2-dihydroisoquinolin-7-yl]oxazolidin-5-ylmethyl methanesulfonate (20.0 mg, 0.0415 mmol) obtained in step C of Example 1-30 was dissolved in acetonitrile (0.1 ml). Thereafter, morpholine (3.6 μl) was added to the obtained solution, and the obtained mixture was stirred under heating to reflux for 22 hours. Thereafter, the reaction solution was cooled to a room temperature, and it was then concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (methylene chloride:methanol=40:1), so as to obtain 7-(5-morpholin-4-ylmethyl-2-oxooxazolidin-3-yl)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one (9.7 mg; yield: 49%) in the form of a colorless amorphous substance.

Provenance & Evidence