反应详情

A solution of 2-chloro-5-(trifluoromethyl)pyrazine (CAS number 799557-87-2; 198 mg, 1.087 mmol), (1S,2S)-1-N,1-N-dibenzyl-2-N-methylcyclopentane-1,2-diamine (291 mg, 0.988 mmol) and DIPEA (518 μl, 2.97 mmol) in DMSO (3.3 ml) was subjected to microwave irradiation at 140° C. for 4 hours. The reaction was diluted with ethyl acetate (20 ml), washed with a saturated solution of sodium bicarbonate (3×20 ml), brine (20 ml), filtered through a hydrophobic frit and concentrated in vacuo. This was then purified by column chromatography (silica, 0-15% ethyl acetate/petrol) to afford the title compound.

1. customirradiation at 140° C. for 4 hours
2. washwashed with a saturated solution of sodium bicarbonate (3×20 ml), brine (20 ml)
3. filtrationfiltered through a hydrophobic frit
4. concentrationconcentrated in vacuo
5. customThis was then purified by column chromatography (silica, 0-15% ethyl acetate/petrol)