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Many compounds of biological and pharmacological interest are as-
metric and show optical activity. Approximately 40% of the drugs in
use are known to be chiral and only about 25% are administered as
pure enantiomers. It is well established that the pharmacological
activity is mostly restricted to one of the enantiomers (eutomer).
In several cases, unwanted side effects or even toxic effects may
occur with the inactive enantiomer (distomer). Even if the side
effects are not that drastic, the inactive enantiomer has to be
meta- lized, which represents an unnecessary burden for the
organism. The admin- tration of pure, pharmacologically active
enantiomers is therefore of great importance. The ideal way to get
to pure enantiomers would be by enantioselective synthesis.
However, this approach is usually expensive and not often
practicable. Usually, the racemates are obtained in a synthesis,
and the separation of the enantiomers on a preparative scale is
necessary. On the other hand, there is also a great demand for
methods of enantiomer separation on an analytical scale for
controlling synthesis, checking for racemization p- cesses,
controlling enantiomeric purity, and for pharmacokinetic studies.
C- ventional methods for enantiomer separation on a preparative
scale are fractionated crystallization, the formation of
diastereomeric pairs followed by repeated recrystallization, and
enzymatic procedures. In recent years, ch- matographic methods such
as gas chromatography and, especially, liquid ch- matography have
attracted increasing interest for chiral separation, both on
analytical and preparative scales.
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