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Chirality is a major concern in the modern pharmaceutical industry. This interest can be attributed largely to a heightened awareness that enantiomers of a racemic drug may have different pharmacological activities, as well as different pharmacokinetic and pharmacodynamic effects. Thus, one isomer may produce the desired therapeutic activities while the other may be inactive or, in worst cases, produce unwanted effects. However, bietamiverine and dipiproverine have been only synthesized as racemic mixtures by transformation of phenylacetic and these are used as antispasmodic and anticholinergic respectively. (Scheme 1).

Synthesis of (R)-(-)-phenylpiperidin-1-yl-acetic acid and its utilization for the synthesis of (R)-(-)-bietamiverine and (R)-(-)-dipiproverine