1,5-Dimethyl 2-methylenepentanedioate → 1-(2,4-Dimethoxybenzyl)-6-oxopiperidine-3-carboxylic Acid Methyl Ester

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Reaction Steps

To a solution of 2-methylenepentanedioic acid dimethyl ester (19.2 g) in toluene (195 ml) was added 2,4-dimethoxybenzylamine (16.6 ml), and the mixture was stirred for 3 days at reflux. This reaction solution was cooled to room temperature, and then washed with a 1M aqueous solution of hydrochloric acid, water and a saturated aqueous solution of sodium chloride, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to give a crude product of the titled compound (26.8 g).

Provenance & Evidence