Stereoselective Crystallization as a Basis for Single‐Enantiomer Drug Production

In the 21st century, single enantiomeric chiral active pharmaceutical ingredients (APIs) prevail among new drugs. Their preparation is made easier by using direct methods for the separation of racemates. The history of this issue is summarized and information about new and updated methods of conglom...

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Bibliographic Details
Published in:Chemical engineering & technology 2017-07, Vol.40 (7), p.1211-1220
Main Authors: Bredikhin, Alexander A., Bredikhina, Zemfira A.
Format: Article
Language:English
Subjects:
Crystallization
Direct resolution
Identification methods
Ingredients
Normal conglomerates
Separation
Single‐enantiomer drugs
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Summary:In the 21st century, single enantiomeric chiral active pharmaceutical ingredients (APIs) prevail among new drugs. Their preparation is made easier by using direct methods for the separation of racemates. The history of this issue is summarized and information about new and updated methods of conglomerate identification and practical implementation options for direct resolutions is provided. Examples are given for the application of direct methods for obtaining enantiopure APIs by the resolution of their racemic synthetic precursors, using a slight modification of the target product and finally by direct resolution of the racemic chiral drugs as such. Nowadays, single enantiomeric chiral active pharmaceutical ingredients dominate among new drugs. Direct methods for the separation of racemates simplify their preparation. A survey is given on the history of this topic as well as information about actual methods of conglomerate identification and practical implementation options for direct resolutions.
ISSN:0930-7516
1521-4125
DOI:10.1002/ceat.201600649