Preparation of ketone amides

Details Preparation of ketone amides Preparation of ketone amides

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01)

Patent

CA 2594106

The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1 -(2,4- dimethylpyrimidine-5-carbonyl)-4-piperidone, 1 -[(2,4-dimethyl-3- pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry. (formule I)

La présente invention concerne un nouveau procédé de préparation de cétone-amides, qui sont des intermédiaires utiles pour la préparation d'antagonistes du récepteur CCR5 et par conséquent utiles pour le traitement de mammifères infectés par le virus du VIH. L'invention concerne spécifiquement un nouveau procédé de synthèse de 1-(2,4-diméthylpyrimidine-5-carbonyl)-4-pipéridone, 1-[(2,4-diméthyl-3-pyridinyl)carbonyl]-4-pipéridone et de composés associés. Une caractéristique importante de l'invention est l'utilisation d'un milieu de réaction à trois phases présentant une phase organique et une suspension tampon saline.

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