p-Toluenesulfonic acid → 4,5-Difluoro-6-(2-fluoro-4-iodo-phenyl)-2-methyl-6,8-dihydro-imidazo[4',5':3,4]benzo[1,2-d]oxazol-7-one

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Reaction Steps

Intermediate I-18a was prepared from 5-amino-6,7-difluoro-1-(2-fluoro-4-iodo-phenyl)-4-hydroxy-1,3-dihydro-benzoimidazol-2-one (I-13a: 550 mg, 1.3 mmol) in 1,1,1-triethoxy-ethane (5 mL) and p-toluene sulfonic acid (20 mg, 0.13 mmol) using procedures analogous to those described above for Intermediate I-16a to afford 310 mg of the product (53.6% yield). H1NMR (DMSO-d6, 300 MHz): δ 12.39 (s, 1H), 7.96 (dd, 1H), 7.78 (d, 1H), 7.48 (t, 1H), 2.67 (s, 3H). LCMS: 92.6%, m/z=445.9 (M+1).

Provenance & Evidence