反应详情

A mixture of tetrahydro-pyrrolo[1,2-a]pyrazine-1,6-dione (compound of Description 15, 150 mg, 0.97 mmol), p-tolyliodide (424 mg, 1.94 mmol), CuI (62 mg, 0.32 mmol) and K2CO3 (134 mg, 0.98 mmol) in dimethylformamide (6 ml) was refluxed for 2 hours. The solvent was removed under vacuum; the residue was triturated with ethyl acetate and after filtering off the insoluble material, the organic layer was washed with brine, dried (Na2SO4) and evaporated under vacuum. The residue was purified by flash chromatography (DCM/MeOH 95/5 respectively) to give the title compound as a light brown powder (70 mg, 30% yield).

1. temperaturewas refluxed for 2 hours
2. customThe solvent was removed under vacuum
3. customthe residue was triturated with ethyl acetate
4. filtrationafter filtering off the insoluble material
5. washthe organic layer was washed with brine
6. dry with materialdried (Na2SO4)
7. customevaporated under vacuum
8. customThe residue was purified by flash chromatography (DCM/MeOH 95/5 respectively)