Toluene → N-[5-(cis-3,5-Dimethyl-1-piperazinyl)-2-(methyloxy)phenyl]-4-(3-thienyl)benzenesulfonamide

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

To a mixture of 4-bromo-N-[5-(cis-3,5-dimethyl-1-piperazinyl)-2-(methyloxy)phenyl]benzenesulfonamide (E106) (200 mg, 0.44 mmol) and 3-thienylboronic acid (113 mg, 0.88 mmol) in DME (3 ml) was added potassium tert-butoxide (445 mg, 3.97 mmol) and tetrakis(triphenylphosphine)palladium(0) (30.5 mg, 0.03 mmol) in water (1 ml) and the resulting mixture stirred in a microwave (set at high absorbance) at 100° C. for 30 minutes. 2-3 ml of toluene added and solvent evaporated, the residue dissolved in methanol and added to a preconditioned (methanol) SCX cartridge eluting with methanol (×3), ammonia (1M in methanol (×2)) and then ammonia (2M in methanol (×3)), followed by by mass directed autoprep HPLC followed by trituration with diethyl ether to afford the title compound (E119). MS (AP+) m/e 458 [M+H]+.

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