Dimethylsulphamoyl chloride → 4,5-Difluoro-6-(2-fluoro-4-iodo-phenyl)-7-oxo-6,7-dihydro-imidazo[4',5':3,4]benzo[1,2-d]oxazole-8-sulfonic acid dimethylamide

Participants

Reaction Steps

Intermediate I-20a was prepared from 4,5-difluoro-6-(2-fluoro-4-iodo-phenyl)-6,8-dihydro-imidazo[4′,5′:3,4]benzo[1,2-d]oxazol-7-one (I-15a: 80 mg, 0.185 mmol), N,N-dimethylaminosulfonyl chloride (41 mg, 0.277 mmol), TEA (78 mg, 0.55 mmol) and DMAP (10 mg) using procedures analogous to those described above for Intermediate I-19a to afford 60 mg of the product (60% yield). H1NMR (CDCl3, 300 MHz): δ 8.16 (s, 1H), 7.72-7.69 (m, 1H), 7.68-7.65 (m, 1H), 7.29-7.22 (m, 1H), 3.2 (s, 6H).

Provenance & Evidence