3-(Methoxymethyl)benzeneboronic acid → N-[5-(cis-3,5-Dimethyl-1-piperazinyl)-2-(methyloxy)phenyl]-3'-[(methyloxy)methyl]-4-biphenylsulfonamide

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

To a mixture of 4-bromo-N-[5-(cis-3,5-dimethyl-1-piperazinyl)-2-(methyloxy)phenyl]benzenesulfonamide (E106) (100 mg, 0.22 mmol) and {3-[(methyloxy)methyl]phenyl}boronic acid (75 mg, 0.45 mmol) in DME (3 ml) was added potassium tert-butoxide (220 mg, 1.96 mmol) and tetrakis(triphenylphosphine)palladium(0) (15 mg, 0.01 mmol) in water (1 ml) and the resulting mixture stirred in a microwave (set at high absorbance) at 100° C. for 30 minutes. The resulting mixture was then evaporated and purified by SCX followed by mass directed autoprep HPLC to afford the title compound (E117). MS (ES+) m/e 496 [M+H]+.

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