Process for synthesizing chiral n-aryl piperazines

C - Chemistry – Metallurgy – 07 – D

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C07D 405/14 (2006.01)

Patent

CA 2477892

A process for formation of N-aryl piperazines with chiral side-chains having the structure shown in formula below, and for making intermediate compounds therefor: (Formula I). In this process, chirality is introduced at the piperazine ring formation step and 2-aminopyridyl substitution is incorporated via displacement. The resulting N,N'-disubstituted piperazines act on the central nervous system at 5HT receptors.

Cette invention a trait à un procédé de préparation de pipérazines N-aryle possédant des chaînes latérales chirales, dont la structure correspond à la formule (I) présentée ci-dessous, ainsi qu'à la production de composés intermédiaires desdites pipérazines. Dans le cadre de ce procédé, on confère la chiralité à ces substances au moment de la formation du noyau de la pipérazine et l'on opère une substitution par aminopyridyle par un déplacement. Les pipérazines N, N' di-substituées agissent sur le système nerveux central au niveau des récepteurs 5HT.

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