Iodine → 6-(6-Chloro-imidazo[1,2-b]pyridazin-3-ylmethyl)-5,7-difluoro-quinoline

Participants

Reaction Conditions

Reaction Steps

(rac)-(6-Chloro-imidazo[1,2-b]pyridazin-3-yl)-(5,7-difluoro-quinolin-6-yl)-methanol (Stage 171.3, 200 mg, 0.577 mmol) was dissolved in acetic acid (4.93 mL) and introduced in a microwave reactor together with iodine (439 mg, 1.731 mmol) and H3PO2 (0.47 mL of a 50% aqueous solution, 8.65 mmol). The RM was stirred under microwave irradiations at 150° C. for 5 min. It was basified by a 2.5 M NaOH solution and extracted twice with EtOAc. The organics were joined and washed with brine, dried over Na2SO4 and the solvent was removed to afford the title compound as a beige solid (tR 1.0 min (conditions 2), MH+=331).

Provenance & Evidence