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Rac- and R-(+)-[4,4′,5,5′-2H4]-2-(1′-[2′′,6′′-dichlorophenoxy]-ethyl)-Δ2-imidazoline (lofexidine)

✍ Scribed by Ashish P. Vartak; Vijayakumar Sonar; Peter A. Crooks

Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
128 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The synthesis of the d~4~‐forms of rac‐ and R‐lofexidine was accomplished. Two methods are described; one method is a two‐step synthesis of rac‐d~4~‐lofexidine from 2‐chloropropionitrile, the second method is a three‐step preparation of R‐d~4~‐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‐d~4~‐ lofexidine. These procedures also conserve the utilization of the relatively expensive [1,1′,2,2′‐^2^H~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 © 2009 John Wiley & Sons, Ltd.

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