1,2-Dichloroethane → 4-[[6-Chloro-3-(4-chloro-2-fluorobenzyl)-2-methylimidazo[1,2-b]pyridazin-8-yl]methyl]morpholine

Participants

Reaction Conditions

Reaction Steps

Combine (4-chloro-2-fluorophenyl)(6-chloro-2-methyl-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-3-yl)methanol (0.4 g, 0.94 mmol), 1,2-dichloroethane (25 mL), triethylsilane (0.45 mL, 3 equiv.), and trifluoroacetic acid (0.57 mL, 8 equiv.) in a round bottom flask and place under nitrogen. Heat at 70° C. overnight. Concentrate reaction in vacuo. Load onto a Varian MegaElut® 10 gram SCX ion exchange cartridge (prewashed with methanol). Elute with methanol to remove non-basic impurities. Elute with 2 M ammonia in methanol. Concentrate in vacuo to give the title compound (0.36 g, 94%). LCMS (4 min)=409.0, 411.0, M+1.

Provenance & Evidence