Tetrahydrofuran → HCID 131735537, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of tert-butyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate (12.0 g, 35.0 mmol) and tetrakis(triphenylphosphine)palladium (2.0 g, 1.7 mmol) in THF (200 mL, dry) was added dropwise a solution of benzylzinc(II) bromide in THF (140 mL, 0.5 M, 70 mmol). The reaction mixture was stirred at 70° C. for 4 h under N2, cooled to RT, then diluted with ethyl acetate (300 mL), filtered and concentrated. The residue was purified by silica gel chromatography, eluting with ethyl acetate/petroleum ether=1/20˜1/10, to give -butyl 4-(5-benzylpyrimidin-2-yl)piperazine-1-carboxylate (7.5 g, yield 60%) as a white solid, MS (ES+) C20H26N4O2 requires: 354, found: 355 [M+H]+.

Provenance & Evidence