2-Chloro-6-Methylphenyl Isothiocyanate → Methyl (2-(2-chloro-6-methylphenylamino)-7-fluoro-6-benzoxazolyl)acetate

참여 물질

반응 단계

Methyl (4-amino-2-fluoro-3-hydroxyphenyl)acetate (1.0 g, 5.02 mmol) was dissolved in methanol (30 ml). To the resulting solution was added 2-chloro-6-methylphenyl isothiocyanate (841 mg, 4.58 mmol) at room temperature. After the resulting mixture was stirred for 5 days, mercuric oxide (yellow) (1.14 g, 4.36 mmol) was added thereto. The mixture was stirred at 70° C. for 23 hours. After cooling, the reaction mixture was filtered through Celite and washed with methanol. The filtrate was distilled under reduced pressure to remove the solvent. The residue was purified by chromatography on a silica gel column, whereby from chloroform/ethyl acetate (30/1) eluate fractions, methyl (2-(2-chloro-6-methylphenylamino)-7-fluoro-6-benzoxazolyl)acetate (1.45 g, 95%) was obtained as a red amorphous substance.

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