Iodine → HCID 178521469, compound

Participants

Reaction Steps

3-[6-(2,4-Difluoro-phenoxy)-1H-indazol-4-yloxy]-propane-1,2-diol (0.45 g, 1.34 mmol) was dissolved in 5 mL of dry DMF, and powdered KOH (0.288 g, 5.1 mmol) was added. The reaction mixture was stirred under nitrogen for 10 minutes at room temperature, and iodine (0.536 g, 2.11 mmol) was added in two portions. The reaction mixture was stirred for 90 minutes. The reaction mixture was partitioned between EtOAc and 5% aqueous sodium bisulfite solution, and the organic layer was separated, dried (MgSO4), filtered and concentrated under reduced pressure. The residue was chromatographed through silica (0%-5% MeOH in dichloromethane) to give 0.408 g of 3-[6-(2,4-difluoro-phenoxy)-3-iodo-1H-indazol-4-yloxy]-propane-1,2-diol, MS(M+H)=436.

Provenance & Evidence