反应详情

温度

100 °C

To a mixture of 4-bromo-2-chloro-N-[5-(cis-3,5-dimethyl-1-piperazinyl)-2-(methyloxy)phenyl]benzenesulfonamide (E104) (220 mg, 0.45 mmol), (5-methyl-2-furanyl)boronic acid (113 mg, 0.90 mmol) and tetrakis(triphenylphosphine)palladium(0) (58 mg, 0.05 mmol) in DME (3 ml) was added potassium tert-butoxide (454 mg, 4.10 mmol) in water (1 ml), and the reaction heated in the microwave (set at high absorbance) at 100° C. for 30 minutes. The reaction was poured on to the SCX column eluting first with methanol and then 2M ammonia in methanol. The basic fractions were combined and solvent evaporated in vacuo. The product was purified by mass directed autoprep HPLC, the relevant fractions collected and solvent evaporated in vacuo. The product was triturated in ether to give the title compound (E306). MS (ES+) m/e 490/492 [M+H]+.

1. additionThe reaction was poured on to the SCX column
2. washeluting first with methanol
3. customsolvent evaporated in vacuo
4. customThe product was purified by mass
5. customthe relevant fractions collected
6. customsolvent evaporated in vacuo
7. customThe product was triturated in ether