反应详情

A suspension of tert-butyl N-[(1S,2S)-2-{[3-bromo-5-(trifluoromethyl)pyrazin-2-yl]amino}cyclopentyl]carbamate (2.44 g, 5.73 mmol), cyclopropylboronic acid (2.46 g, 28.6 mmol), potassium carbonate (3.17 g, 22.9 mmol) and tetrakis(triphenylphosphine)palladium (0.662 g, 0.57 mmol) in 1,4-dioxane (15 ml) and water (4 ml) was subjected to microwave irradiation at 140° C. for 2 hours. The reaction was partitioned between ethyl acetate (20 ml) and water (20 ml). The aqueous layer was extracted with ethyl acetate (2×50 ml) and combined organics were washed with brine (50 ml), filtered through a hydrophobic frit and concentrated in vacuo. The crude product was purified by column chromatography (silica, 0-50% ethyl acetate/petrol) to afford the title compound.

1. customirradiation at 140° C. for 2 hours
2. customThe reaction was partitioned between ethyl acetate (20 ml) and water (20 ml)
3. extractionThe aqueous layer was extracted with ethyl acetate (2×50 ml)
4. washcombined organics were washed with brine (50 ml)
5. filtrationfiltered through a hydrophobic frit
6. concentrationconcentrated in vacuo
7. customThe crude product was purified by column chromatography (silica, 0-50% ethyl acetate/petrol)