PREPARATION OF ACID AMIDE
PURPOSE:To obtain an acid amide useful as an anticonvulsant and a hypnotic in high yield without preparing by-products, by reacting an organic acid ester with ammonia or an amine in the presence of an alcoholate of an alkali metal. CONSTITUTION:A bicyclo[2,2,1]heptene-5-carboxylic acid ester-2 shown...
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Zusammenfassung: | PURPOSE:To obtain an acid amide useful as an anticonvulsant and a hypnotic in high yield without preparing by-products, by reacting an organic acid ester with ammonia or an amine in the presence of an alcoholate of an alkali metal. CONSTITUTION:A bicyclo[2,2,1]heptene-5-carboxylic acid ester-2 shown by the formula (R is alkyl, aryl or aralkyl) is reacted with ammonia or a primary amine or secondary amine (e.g., methylamine, ethylamine, aniline, pyridine, etc.) in the presence of an alcoholate of an alkali metal (e.g., NaOCH3) at 10-150 deg.C, preferably at 40-100 deg.C, to give bicyclo[2,2,1]heptene-5-carboxylic acid amide-2. The amount of the alcoholate of an alkali metal used is preferably 5-20mol% based on the ester. |
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