Process for the preparation of indole derivatives or salts...

Details Process for the preparation of indole derivatives or salts... Process for the preparation of indole derivatives or salts...

C - Chemistry, Metallurgy

07

D

C07D 209/12 (2006.01)

Patent

CA 2382116

A novel process for preparing 3-acylindoles or salts thereof in high yields, which comprises adding a Grignard reagent prepared by reacting an alkyl halide with magnesium in a hydrocarbon solvent in the presence of a base to indole or a salt thereof under cooling to activate the indole or salt and reacting the intermediate obtained by this activation with an acylating agent under cooling to thereby obtain a 3-acylindole or a salt thereof.

L'invention porte sur un nouveau procédé à fort rendement de préparation de 3-acylindoles ou de leurs sels consistant à ajouter un réactif de Grignard, préparé en faisant réagir un halogénure d'alkyle avec du magnésium dans un solvant d'hydrocarbure en présence d'une base, avec de l'indole ou l'un de ses sels, en refroidissant pour activer l'indole ou son sel, puis à faire réagir en refroidissant l'intermédiaire obtenu par cette activation avec un agent acylant, ce qui donne le 3-acylindole ou l'un de ses sels.

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