Carbon Tetrachloride → HCID 59520039, compound

Participants

Reaction Conditions

Reaction Steps

The 7-((R)-5-hydroxymethyl-2-oxooxazolidin-3-yl)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one (150 mg, 0.37 mmol) obtained in step B of Example 1-14 was dissolved in acetonitrile (5 ml). Thereafter, N,N-diisopropylethylamine ml, 2.96 mmol), carbon tetrachloride (0.706 ml, 7.4 mmol), N,N-dimethylaminopyridine (14 mg, 0.22 mmol), and dibenzyl phosphite (0.410 ml, 1.86 mmol) were added to the solution. The obtained mixture was stirred at 50° C. for 15 hours. Thereafter, the reaction mixture was concentrated under reduced pressure. The obtained residue was purified by silica gel chromatography (hexane:ethyl acetate=1:5), so as to obtain phosphate dibenzyl ester (R)-2-oxo-3-[1-oxo-3-(2-trifluoromethylphenyl)-1,2-dihydroisoquinolin-7-yl]-oxazolidin-5-ylmethyl ester (85 mg, 34%) in the form of a colorless foaming substance.

Provenance & Evidence