Potassium Carbonate → (4-((4-Acetylpiperazin-1-yl)methyl)phenyl)boronic acid

反応式

Br[C:2]1[CH:7]=[CH:6][C:5]([B:8]2[O:12]C(C)(C)C(C)(C)[O:9]2)=[CH:4][CH:3]=1.[C:17](=O)([O-])[O-].[K+].[K+].[C:23]([N:26]1[CH2:31][CH2:30][NH:29][CH2:28][CH2:27]1)(=[O:25])[CH3:24]>CN(C=O)C>[C:23]([N:26]1[CH2:31][CH2:30][N:29]([CH2:17][C:2]2[CH:3]=[CH:4][C:5]([B:8]([OH:9])[OH:12])=[CH:6][CH:7]=2)[CH2:28][CH2:27]1)(=[O:25])[CH3:24]

参加物

実験手順

To a stirred mixture of 2-(4-bromophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (0.120 g, 0.4 mmol) and potassium carbonate (0.056 g, 0.4 mmol) in DMF (3 mL) was added N-acetylpiperazine (0.052 g, 0.4 mmol) and the resulting reaction mixture stirred at room temperature for 2 hours. The solvent was removed in vacuo. The residue was suspended in MeOH and purified by SPE using an MP-TsOH resin (1000 mg) cartridge to afford 4-((4-acetylpiperazin-1-yl)methyl)phenylboronic acid as an oil which was used without further purification. LCMS (1) Rt: 1.04 min; m/z (ES+) 263.