反应详情

A mixture of tert-butyl N-[(1S,2S)-2-{[3-bromo-5-(trifluoromethyl)pyrazin-2-yl]amino}cyclopentyl]carbamate (800 mg, 1.88 mmol), methylboronic acid (CAS number 13061-96-6; 338 mg, 5.64 mmol), tetrakis(triphenylphosphine)palladium (217 mg, 0.19 mmol) and, 2 M potassium carbonate (aq, 3.8 ml, 7.53 mmol) in 1,4-dioxane (6.3 ml) was sealed, evacuated and purged with nitrogen and then subjected to microwave irradiation at 120° C. for 2 hours. The reaction mixture was then diluted with ethyl acetate (40 ml) and water (10 ml). The organics were washed with water and brine, dried over sodium sulfate and concentrated in vacuo. The residue was then purified by column chromatography (silica, 0-50% ethyl acetate/petrol) to afford the title compound.

1. customwas sealed
2. customevacuated
3. custompurged with nitrogen
4. customirradiation at 120° C. for 2 hours
5. additionThe reaction mixture was then diluted with ethyl acetate (40 ml) and water (10 ml)
6. washThe organics were washed with water and brine
7. dry with materialdried over sodium sulfate
8. concentrationconcentrated in vacuo
9. customThe residue was then purified by column chromatography (silica, 0-50% ethyl acetate/petrol)