1-(Prop-2-yn-1-yl)pyrrolidin-2-one → HCID 23509810, compound

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Reaction Steps

The desired compound was prepared by the method of Example 8 from 300 mg (2.11 mmol) of 1-methyl-piperidin-3-carbaldehyde oxime prepared in Example 5 and 520 mg (2 equivalents) of 1-propargyl pyrrolidin-2-one prepared in Example 7, and purified by separation with silica gel column chromatography using chloroform/methanol (gradient of 20:1 to 10:1) as eluent to obtain 278.1 mg (50% yield) of 1-[3-(1-methyl-piperidin-3-yl)-isoxazol-5-yl-methyl]-pyrrolidin-2-one. Subsequently, 1:1 acid addition salt with oxalic acid was obtained from the diethyl ether solution.

Provenance & Evidence