4,5-Dichlorophthalic anhydride → (Z)-5,6-dichloro-3-(4-fluoro-3-(4-methoxypiperidine-1-carbonyl)benzylidene)isobenzofuran-1(3H)-one

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A flask charged with 5,6-dichloroisobenzofuran-1,3-dione (370 mg, 1.71 mmol), 2-(4-fluoro-3-(4-methoxypiperidine-1-carbonyl)phenyl)acetic acid (43) (496 mg, 1.68 mmol) and Sodium acetate (34 mg, 0.41 mmol) was lowered into a pre-heated aluminium block at 210° C. The resulting mixture was heated further and stirred at 240° C. for 1 hour then cooled. The residue was triturated, with sonication, under ethanol (˜25 mL) and solid collected by suction filtration to afford crude product (128 mg, 16.92%), which was used directly without further purification; m/z (LC-MS, ESI+), RT=2.79 (M+H 450.1 & 452.0).

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