6-Chloro-3-Benzofuranone → (5R)-5-(5-(6-chloro-2,3-dihydrobenzofuran-3-ylamino)-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepane-3-thione

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Reaction Steps

Prepared in an analogous manner as described for intermediate A22A from (R)-5-(5-amino-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepane-3-thione (intermediate A19B) (96 mg, 302 μmol) and commercially available 6-chlorobenzofuran-3(2H)-one [CAS no 3260-78-4] (61.0 mg, 362 μmol) The (5R)-5-(5-(6-chloro-2,3-dihydrobenzofuran-3-ylamino)-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepane-3-thione (72 mg, 153 μmol, 50.7% yield) was obtained as a light yellow foam. MS (ISN): m/z=469.1 [(M−H)−] and 471.2 [(M+2-H)−].

Provenance & Evidence