Iodine → (Rac)-6-[1-(6-chloro-imidazo[1,2-b]pyridazin-3-yl)-ethyl]-5,7-difluoro-quinoline

Participants

Reaction Steps

(rac)-1-(6-Chloro-imidazo[1,2-b]pyridazin-3-yl)-1-(5,7-difluoro-quinolin-6-yl)-ethanol (Stage 182.2, 570 mg, 1.58 mmol), iodine (1.203 g, 4.74 mmol) and H3PO2 (1.293 mL of a 50% aqueous solution, 23.7 mmol) were charged together with acetic acid (16 mL) in a microwave vial. The mixture was subjected to MW-irradiation at 150° C. for 5 min. It was then taken up with water and basified with NaOH (2.5 M). It was extracted with EtOAc twice and the organics were joined and washed with brine, dried over Na2SO4 and the solvent was removed. The title compound was obtained as a yellow solid (tR 1.1 min (conditions 2), MH+=346).

Provenance & Evidence