Process for preparation of a salt of .gamma.-(piperidyl)...

Details Process for preparation of a salt of .gamma.-(piperidyl)... Process for preparation of a salt of .gamma.-(piperidyl)...

C - Chemistry, Metallurgy

07

D

C07D 211/34 (2006.01) C07D 213/55 (2006.01)

Patent

CA 2239138

At least one of a Rh catalyst, a Pd catalyst or a Ru catalyst is used as a catalyst in preparing the salt of .gamma.-(piperidyl)-butyric acid (2) by hydrogenating the salt of .gamma.-(pyridyl)butyric acid (1) [preferably the salt of y-(pyridyl)butyric acid (1) obtained in the undermentioned steps (a) and (b) and containing not more than 3% by weight of salt of bis(pyridylethyl)acetic acid (3)] in a solvent in the presence of a catalyst: (a) reacting the vinylpyridine (4) with the diester of malonic acid (5) in the presence of a base to give the 2-(pyridylethyl)malonic acid diester (6), and (b) hydrolyzing and decarboxylating the 2- (pyridylethyl)malonic acid diester (6) obtained in the step (a) in an acidic aqueous solution to give the salt of .gamma.-(pyridyl)butyric acid (1).

L'invention a trait à un procédé de préparation de sels acides (2) d'acide gamma -(pipéridyl)butyrique par l'hydrogénation d'un sel acide (1) d'acide gamma -(pyridyl)butyrique (préparé, de préférence, en respectant les étapes (a) et (b) et avec une concentration en sels acides (3) d'acide acétique bis(pyridyléthyl) n'excédant pas 3 en pourcentage pondéral) dans un solvant en présence d'un catalyseur, qu'il s'agisse de rhodium, de palladium ou de ruthénium. Etape a: faire réagir un composé à base de vinylpyridine (4) avec un diester (5) d'acide malonique en présence d'une base afin de produire un diester (6) d'acide malonique 2-(pyridyléthyl). Etape b: hydrolyser et décarboxyler dans une solution aqueuse d'acide le diester (6) obtenu grâce aux opérations menées dans l'étape (a) afin de préparer le sel acide (1) d'acide gamma -(pyridyl)butyrique.

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