3-(4-Piperidyl)-6-fluoro-1,2-benzisoxazole → HCID 17943138, compound

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Reaction Conditions

Reaction Steps

A stirred mixture of 4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidine (5.5 g, 25 mmol) and 1,2-expoxybutane (1.89 g, 26.3 mmol) in isopropyl alcohol (100 ml) was heated at 65° C. for 2 days. This mixture was cooled and the solvent was removed to leave a brown oil which was purified by flash chromatography over a silica gel column (SiO2, 70 g; eluted with DCM, 1 l and MeOH:DCM 2%: 98%) to give an off-white solid weighing 6.3 g. Recrystallization from hot ethanol yielded 1.96 g of fine crystals, m.p. 87°-88° C. ANALYSIS: Calculated for C16H21FN2O2 : 65.73%C 7.24%H 9.58%N Found: 65.83%C 7.12%H 9.54%N

Provenance & Evidence