Process for the preparation of a piperazine derivative

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01) C07C 209/74 (2006.01) C07C 211/29 (2006.01) C07C 213/04 (2006.01) C07C 215/30 (2006.01) C07D 213/85 (2006.01) C07D 241/04 (2006.01)

Patent

CA 2351528

A process for preparing a piperazine derivative represented by the formula~ (V): (see figure I) comprising reacting 1-methyl-3-phenylpiperazine with 2-chloro-3-cyanopyridine in an aprotic polar organic solvent in the presence of a base and an alkali metal halide. The piperazine derivative and its oxalate are compounds useful as preparation intermediates of mirtazapine.

L'invention concerne un procédé de préparation d'un dérivé piperaziné représenté par la formule (V). le procédé consiste à faire réagir 1-méthyl-3-phénylpipérazine avec 2-chloro-3-cyanopyridine en présence d'une base et d'un halogénure de métal alcalin dans un solvant organique polaire aprotique. Ledit dérivé et son oxalate sont utiles comme intermédiaires pour la préparation de mirtazapine.

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