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US 7,256,289 B2Granted
Process for making chiral 1,4-disubstituted piperazines
AssigneeWyeth
InventorsIvo Ladislav Jirkovsky, Joseph Zeldis, Gregg Brian Feigelson
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Abstract
A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: 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. The intermediate compounds of Formula II and IV as set forth herein are also included.
Claims3
A compound of formula IV
- wherein R is C1–C3-alkyl and Ar represents dihydro-benzodioxinyl or benzodioxinyl, and the optical isomers thereof.
A compound selected from the group consisting of
- (R)-4-(2,3-dihydro-1,4-benzodioxin-5-yl)-β-methyl-1-piperazineethanol;
- and,
- (R)-4-(2,3-dihydro-1,4-benzodioxin-5-yl)-β-ethyl-1-piperazineethanol and the optical isomers thereof.
Dependencies are inferred from the claim text.