反应详情

A mixture of N-[(1S,2S)-2-{[3-chloro-5-(trifluoromethyl)pyrazin-2-yl]amino}cyclopentyl]-2-(2H-1,2,3-triazol-2-yl)benzamide (Intermediate 29; 170 mg, 0.38 mmol), cyclopropylboronic acid (CAS number 411235-57-9; 97 mg, 1.13 mmol), potassium carbonate (aq. 2 M, 752 μl, 1.51 mmol) and tetrakis(triphenylphosphine)palladium (44 mg, 0.038 mmol) in 1,4-dioxane (1.3 ml) was sealed, purged and evacuated with nitrogen and then subjected to microwave irradiation 120° C. for 1 hour. The reaction was partitioned between ethyl acetate and water, washed with water, brine, dried over magnesium sulfate and concentrated in vacuo. This was then purified by reverse phase preparative HPLC (eluted with acetonitrile/water containing 0.1% ammonia) to afford the title compound.

1. customwas sealed
2. custompurged
3. customevacuated with nitrogen
4. customirradiation 120° C. for 1 hour
5. customThe reaction was partitioned between ethyl acetate and water
6. washwashed with water, brine
7. dry with materialdried over magnesium sulfate
8. concentrationconcentrated in vacuo
9. customThis was then purified by reverse phase preparative HPLC (eluted with acetonitrile/water containing 0.1% ammonia)