Lawesson's reagent → (R)-5-[5-(3-chloro-phenylethynyl)-2-fluoro-phenyl]-6,6-difluoro-5,7,7-trimethyl-[1,4]oxazepan-3-thione

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Reaction Steps

The reaction of (R)-5-[5-(3-chloro-phenylethynyl)-2-fluoro-phenyl]-6,6-difluoro-5,7,7-trimethyl-[1,4]oxazepan-3-one (233 mg, 552 μmol) with Lawesson's reagent (230 mg, 552 μmol) in 1,4-dioxane (15 ml) yielded the (R)-5-[5-(3-chloro-phenylethynyl)-2-fluoro-phenyl]-6,6-difluoro-5,7,7-trimethyl-[1,4]oxazepan-3-thione (129 mg, 53% yield) as a light yellow foam. MS (ISP): m/z=438.1 [M+H]+ and 440.2 [M+2+H]+.

Provenance & Evidence