反应详情

200 mg (0.97 mmol) of 1-azabicyclo[2.2.2]oct-3-ylacetic acid hydrochloride are heated under reflux in 2 ml (27.42 mol) of thionyl chloride for 2 h. The mixture is then freed of excess thionyl chloride in vacuo, and the residue is taken up in 4 ml of DMF. 0.54 ml (3.89 mmol) of triethylamine, 59.4 mg (0.4 mmol) of DMAP and 183.0 mg (0.97 mmol) of 8-nitro-2-naphthylamine are added to this solution. After reaction overnight and purification by preparative HPLC, the resulting product fractions are mixed with 1 M hydrochloric acid and concentrated in vacuo. Recrystallization, of the residue from isopropanol and drying under high vacuum result in 59 mg (15% of theory) of the title compound.

1. customAfter reaction overnight and purification by preparative HPLC
2. concentrationconcentrated in vacuo
3. customRecrystallization
4. dry with materialof the residue from isopropanol and drying under high vacuum