反应详情

Purified water (0.01 ml) and TFA (0.01 ml) were added to a dichloromethane solution that contained the 7-((R)-5-hydroxymethyl-2-oxooxazolidin-3-yl)-3-diethoxymethyl-2H-isoquinolin-1-one (3.3 mg, 0.009 mmol) prepared in step C. The obtained mixture was left at a room temperature for 30 minutes, and the reaction solution was concentrated. The obtained yellow solid and an ethanol solution that contained N-ethyl-1,2-benzenediamine (1.2 mg, 0.009 mmol), which was a known compound described in a publication (Leicester Polytech; Synthetic Communications, vol. 19(7-8), p. 1381, (1989)), were heated to reflux for 17 hours. Thereafter, the reaction solution was concentrated. The obtained residue was purified by preparative silica gel TLC (dichloromethane:methanol=20:1), so as to obtain 3-(1-ethyl-1H-benzoimidazol-2-yl)-7-((R)-5-hydroxymethyl-2-oxooxazolidin-3-yl)-2H-isoquinolin-1-one (2.7 mg, yield: 74%) in the form of a yellow solid.

1. customPurified water (0.01 ml) and TFA (0.01 ml)
2. additionwere added to a dichloromethane solution that
3. concentrationthe reaction solution was concentrated
4. temperaturewere heated
5. temperatureto reflux for 17 hours
6. concentrationThereafter, the reaction solution was concentrated
7. customThe obtained residue was purified by preparative silica gel TLC (dichloromethane:methanol=20:1)