Synthesis of intermediates useful in preparing...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/12 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2293709

The invention relates to a process for preparing a compound of formula (I), comprising: (a) reacting 2,5-dibromo-3-methylpyridine with an amine of the formula NHR5R6 to obtain an amide; (b) reacting the amide with a compound of formula (3) in the presence of a strong base to obtain a compound of formula (4); (c) converting a compound of formula (4) to the corresponding cyano compound or aldehyde; (d) reacting the cyano compound or aldehyde with a piperidine derivative to obtain an aldehyde or alcohol of formula (7a) or (7b), respectively; (e) cyclizing a compound of formula (7a) or (7b); wherein R1-R7 are as defined in the specification.

L'invention concerne un procédé de préparation d'un composé de la formule (I), qui consiste à: a) mettre en réaction 2,5-dibromo-3-méthylpyridine avec un amine de la formule NHR?5¿R?6¿ pour obtenir un amine; b) mettre en réaction l'amine avec un composé de la formule (3) en présence d'une base forte pour obtenir un composé de la formule (4); c) transformer un composé de la formule (4) en composé cyano ou en aldéhyde correspondant; d) mettre en réaction le composé cyano ou l'aldéhyde avec un dérivé de pipéridine pour obtenir un aldéhyde ou un alcool de la formule (7a) ou de la formule (7b), respectivement; e) cycliser un composé de la formule (7a) ou de la formule (7b) dans laquelle R?1¿-R?7¿ sont tels que définis dans le mémorandum descriptif.

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