Researchers at IIT Delhi Develop Catalytic Technology for Sustainable Production of Chiral Active Pharmaceutical Ingredients


India is heavily dependent on the import (~ 85%) of active pharmaceutical ingredients (APIs), and a significant proportion of these APIs are chiral molecules, which are essential building blocks for the production of pharmaceuticals, agrochemicals and chemicals. biologically active compounds.

A research group from IIT Delhi led by Professor Kuntal Manna of the Department of Chemistry and his doctoral students – Neha Antil and Rajashree Newar – have developed catalytic technology for the sustainable and economical synthesis of chiral molecules. The Scientific and Technical Research Council (SERB), a statutory body of the Department of Science and Technology (DST) of the Indian government, funded this research work.

Chiral molecules exist as paired stereoisomers, called enantiomers, which mirror images of each other. 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 can be harmful, while the other form is the desired active ingredient for the drug. Therefore, it is imperative that the predicted API be present in an enantiomerically pure form in the drug.

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

Unfortunately, both methodologies are expensive and not very environmentally friendly. To solve this problem, the research team developed a metal-organic framework (MOF) -based catalytic technology using inexpensive natural raw materials and abundant metals for the sustainable and economical synthesis of enantiomerically pure chiral molecules.

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

The work has been published in reputable journals such as Angewandte Chemie International Edition, 60, 10964-10970 (2021) and ACS Catalysis, 11, 10450-10459 (2021).

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