反应详情

温度

150 °C

A mixture of 6-butyl-8-(4-piperidinyloxy)quinoline (for example, as prepared for Intermediate 4) (65 mg, 0.23 mmol), sodium iodide (47 mg, 0.3 mmol), sodium bicarbonate (190 mg, 2.2 mmol) and 4-bromobutyl 1,1-dimethylethyl sulfone (for example, as prepared for Intermediate 22) (94 mg) in DMF (2 ml) was heated in a Smith Creator™ microwave oven at 150° C. for 20 min. The reaction mixture was applied to an SCX-2 cartridge (10 g), preconditioned with methanol, and eluted with methanol, followed by 10% aqueous 0.88 s.g. ammonia in methanol. The ammoniacal fractions were combined and concentrated in vacuo and the residue (100 mg) was purified by MDAP to give the title compound (58 mg, 46%): LCMS RT=2.65 min, ES+ve m/z 461 (M+H)+.

1. washeluted with methanol
2. customfollowed by 10% aqueous 0.88 s
3. concentrationconcentrated in vacuo
4. customthe residue (100 mg) was purified by MDAP