Hydrochloric Acid → cis-2-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-piperidinyl]propyl]-hexahydro-1H-isoindole-1,3-dione hydrochloride

関与物質

反応手順

A mixture of 1-(3-aminopropyl)-4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidine (3.01 g, 10.8 mmol) and cis-1,2-cyclohexane-dicarboxylic anhydride (1.9 g, 12.3 mmol) in dry pyridine (30 ml) was heated at reflux for 16 hours. The dark brown solution was concentrated to dryness on a rotary evaporator. The crude residue was purified twice by flash chromatography over a silica gel column. The pure product thus obtained weighed 2.5 g (67%). This was converted to the hydrochloride salt by treatment with HCl in ethanol (50 ml). The cis-2-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propyl]-hexahydro-1H-isoindole1,3-dione hydrochloride crystals so obtained weighed 3.0 g, m.p.=242°-245° C.

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