Hydrochloric Acid → 8-(2-chlorophenylamino)-6,7-difluoro-4-methyl-2H-phthalazin-1-one

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Reaction Steps

To a solution of 6-acetyl-2-(2-chlorophenylamino)-3,4-difluorobenzoic acid (62 mg, 0.19 mmol, prepared by the procedures described in Example 1) and hydrazine monohydrate (0.031 mL, 0.63 mmol) in THF (3 mL) was added catalytic amount of 1 N aqueous HCl (0.15 mL, 0.15 mmol) at room temperature. After stirring for 16 hours at room temperature, the reaction mixture was diluted with EtOAc, and washed with water (2×) and brine. The organic layer was dried over MgSO4, filtered, and concentrated in vacuo to give the desired product (53 mg, 86%) that was used directly without further purification.

Provenance & Evidence