反应详情

To a suspension of 2-bromopyrimidine (175 mg, 1.1 mmols), dichlorobis(triphenylphosphine)palladium(II) (35 mg, 0.05 mmols) and Cul (10 mg, 0.05 mmols) was added a solution of 4-ethynyl-piperidine-1-carboxylic acid tert-butyl ester (209 mg, 1 mmol). The mixture was stirred overnight, filtered through Celite, concentrated. The residue was partitioned between ethyl acetate and water, organic layer was isolated, dried (MgSO4), and concentrated. The residue was chromatographed on silica gel eluting with ethyl acetate in hexanes (1:1) to give un-reacted 2-bromopyrimidine (130 mg), then the title compound (23 mg). LCMS m/e (288, M+H).

1. filtrationfiltered through Celite
2. concentrationconcentrated
3. customThe residue was partitioned between ethyl acetate and water
4. customorganic layer was isolated
5. dry with materialdried (MgSO4)
6. concentrationconcentrated
7. customThe residue was chromatographed on silica gel eluting with ethyl acetate in hexanes (1:1)
8. customto give