Process for making chiral 1,4-disubstituted piperazines

C - Chemistry – Metallurgy – 07 – D

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C07D 405/04 (2006.01) C07C 229/12 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2477906

A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula (I) wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

L'invention concerne une méthode de préparation stéréosélective de nouveaux dérivés chiraux d'azote de la moutarde utiles pour synthétiser des pipérazines 1,4-disubstitués, optiquement actifs, de la formule (I), dans laquelle R, Ar et Q sont tels que définis dans le mémorandum descriptif. Elle concerne également des composés intermédiaires obtenus à partir desdits dérivés. Les pipérazines 1,4-disubstitués agissent comme agents de liaison aux récepteurs 5HT1A et sont utiles dans le traitement de troubles du système nerveux central (SNC).

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