Iodine → 6-(1-(6-Chloroimidazo[1,2-b]pyridazin-3-yl)ethyl)-7-fluoroquinoline

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-(6-chloroimidazo[1,2-b]pyridazin-3-yl)-1-(7-fluoroquinolin-6-yl)ethanol (420 mg, 1.10 mmol) in acetic acid (20 mL) was added phosphinic acid (50% aqueous solution, 0.60 ml, 5.51 mmol) and iodine (700 mg, 2.76 mmol). The resulting solution was heated at 110° C. overnight and the solvent was removed. The residue was diluted with water and pH was adjusted to 8-10 with 6N NaOH solution. The mixture was then extracted by CH2Cl2, washed with brine, dried over anhydrous Na2SO4 and concentrated in vacuo. The residue was purified by column chromatography (3% to 10% MeOH in CH2Cl2) to afford 260 mg (yield: 72%) title compound. LCMS (method B): [MH]+=327, tR=2.52 min.

Provenance & Evidence