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Resolution of the Chiral Drugs
Authors:DENG Jingen  ZHU Jin
Abstract:Chiral drugs are generally not permitted to be used in racemic form so that unintended side effects and unnecessary environmental hazards are avoided. Moreover, homochiral molecules are required immediately to progress key toxicological and clinical studies in the drug discovery. One series of technologies which can rapidly supply homochiral compounds is the separation of racemates, and of those the technique of crystallization of diastereomers is extremely effective-principally because it is simple to operate and it affords both enantiomers. In classical resolution via diastereoisomeric salt formation, the resolved compounds are limited to a given racemic acid or base and the choice of a suitable resolving agent for a racemic target compound is achieved by time-consuming trial-and-error procedure.
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