78302-27-9Relevant articles and documents
Rac- and R-(+)-[4,4′,5,5′-2H4]-2- (1′-[2″,6″-dichlorophenoxy]-ethyl)-Δ2- imidazoline (lofexidine)
Vartak, Ashish P.,Sonar, Vijayakumar,Crooks, Peter A.
scheme or table, p. 431 - 434 (2010/07/05)
The synthesis of the d4-forms of rac- and R-lofexidine was accomplished. Two methods are described; one method is a two-step synthesis of rac-d4-lofexidine from 2-chloropropionitrile, the second method is a three-step preparation of R-d4-lofexidine in absolute enantiomeric purity from S-methyl lactate. The commercial availability of R-methyl lactate makes this latter enantioselective synthesis applicable also to the synthesis of S-d4- lofexidine. These procedures also conserve the utilization of the relatively expensive [1,1′,2,2′-2H 4]ethylene diamine precursor. The availability of S- and R-d 4-lofexidines will enable pharmacokinetic studies to be carried out to determine if differential in vivo metabolism of the two enantiomers of lofexidine occurs. Copyright
Imidazoline derivatives and processes for the production thereof
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, (2008/06/13)
2-[α-(2,6-DICHLOROPHENOXY)-ETHYL]-Δ2 -IMIDAZOLINE, AND PHYSIOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, WHICH PROVIDE VASOACTIVITY AND HYPOTENSIVE ACTIVITY.