
BACKGROUND
The majority of pharmaceutical active ingredients are chiral in nature, existing as two or more enantiomers. The US FDA requires companies to produce pure single enantiomers as drugs, or test the toxicity of any enantiomers persisting in the marketed product. There is therefore extensive pressure to develop catalysts with high selectivity for particular enantiomers, in enantiomeric excess (ee). The measurement of ee from test reactions is time consuming, requiring liquid chromatography over chiral supports. There is strong incentive to develop rapid methods of screening for ee, both to detect new enantiomeric compounds and screen new catalysts from libraries or developmental programs.
DESCRIPTION OF THE INVENTION
Our inventors have developed a new method for screening for ee which is colorimetric, rapid and sensitive. The presence of a predetermined enantiomer causes a pronounced color shift which is readily detectable by eye. The reagents are easy to prepare using inexpensive and standard chemical methods, and can be tailored to a wide range of molecules of similar functionality. No separation or enrichment of enantiomers is needed. The guest-host aspect of the invention allows for rapid testing of similar compounds.
The tests have been reduced to practice using naproxen as a model compound.
POTENTIAL ADVANTAGES/USES
DEVELOPMENT STAGE: Proof of principle
SECTOR: Pharmaceuticals, Fine Chemicals
REFERENCE NUMBER: UWO-AG-049
PCT patent application filed
Available for out-licensing. A collaborative research approach involving the inventor would also be considered.