Improved method for the synthesis of substituted...

C - Chemistry – Metallurgy – 07 – C

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C07C 209/46 (2006.01)

Patent

CA 2695203

An improved method for the synthesis of substituted formylamines and substituted amines via an accelerated Leuckart reaction. The Leuckart reaction is accelerated by reacting formamide or N-alkylformamide and formic acid with an aldehyde or a ketone at a preferred molar ratio that accelerates the reaction. The improved method is applicable to various substituted aldehydes and ketones, including substituted benzaldehydes. An accelerated method for the hydrolysis of substituted formylamines into substituted amines using acid or base and a solvent at an elevated temperature. The improved method is useful for the accelerated synthesis of agrochemicals and pharmaceuticals such as vanillylamine, amphetamine and its analogs, and formamide fungicides.

L'invention concerne un procédé amélioré de synthèse de formylamines substituées et d'amines substituées par une réaction de Leuckart accélérée. La réaction de Leuckart est accélérée en faisant réagir des formamide ou un N-alkylformamide et de l'acide formique avec un aldéhyde ou une cétone à un rapport molaire préféré qui accélère la réaction. Le procédé amélioré est applicable à divers aldéhydes ou cétones substitués, y compris des benzaldéhydes substitués. Un procédé accéléré d'hydrolyse de formylamines substituées en amines substituées en utilisant un acide ou une base et un solvant à une température élevée est proposé. Le procédé amélioré est utile pour la synthèse accélérée de produits agrochimiques et de produits pharmaceutiques tels que la vanillylamine, l'amphétamine et ses analogues, et les fongicides à base de formamide.

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