IIT Delhi develops low-cost technology to produce chiral pharmaceutical ingredients

The Science and Engineering Research Board (SERB), a statutory body of the Department of Science and Technology (DST), Government of India, has funded the research work.  

An IIT Delhi research group led by Prof Kuntal Manna from the Department of Chemistry and his PhD students --Neha Antil and Rajashree Newar-- has developed a catalytic technology for the sustainable and economical synthesis of chiral molecules. The Science and Engineering Research Board (SERB), a statutory body of the Department of Science and Technology (DST), Government of India, has funded the research work.  

Active pharmaceutical ingredients explained 

Active pharmaceutical intermediate molecules or API’s are the biologically active, highly potent ingredients in pharmaceutical drugs. These potent ingredients are usually present in enantiomeric form and in most cases one enantiomeric form may be harmful while the other form is the intended active ingredient for the drug. Therefore, it is imperative that the intended active pharmaceutical intermediate is present in pure form in the drug.  

“The developed catalytic technology may play a crucial role in decreasing the country’s dependence on the import of the active pharmaceutical ingredients, which also means lowering of the input cost for the industry that would encourage it to pass on the benefit to the society,” said Prof Manna.  

What are chiral molecules? 

In chemistry, when a molecule can have an exact mirror images of itself and be non-superimposable, it is referred to as chiral. Chiral molecules exist as paired stereoisomers, known as enantiomers, that form mirror images of each other. The classical synthesis of chiral small molecule APIs results in mixtures of paired enantiomers. 

However, two enantiomeric forms of a chiral API exhibit different biological properties, efficacies, and toxicities. One enantiomeric form may be harmful, while the other form is the desired active ingredient for the drug. Therefore, it is imperative that the intended API should be present in enantiomerically pure form in the drug.  

In the pharmaceutical industry, the single enantiomers of chiral APIs are produced by separating the enantiomeric mixture or directly converting the raw material to the desired enantiomer selectively using a catalyst. The industrially used catalysts for such enantioselective transformations are mostly homogeneous and composed of expensive chiral ligands and precious and toxic metals such as iridium, ruthenium, palladium, or rhodium.  

Unfortunately, both methodologies are costly and not eco-friendly. To tackle this problem, the research team developed a Metal-Organic Frameworks (MOFs) based catalytic technology using inexpensive natural feedstocks and abundant metals for the sustainable and economical synthesis of enantiomerically pure chiral molecules.  

Prof Manna believes that the development of MOF-based earth-abundant metal catalysts has the potential for cost-effective and environmentally benign domestic production of enantiopure chiral APIs. 

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