New chemistry method simplifies late-stage modification of drug molecules

Chemists at The Scripps Research Institute (TSRI) have invented a technique that overcomes a long-standing problem in organic chemistry and should streamline the process of discovery and development for many new drugs.

The technique, known as ligand-accelerated non-directed C–H functionalization, is expected to find application not just in the pharmaceutical chemistry industry but also in a wide range of other chemical industries. However, it should be particularly useful for altering complex candidate drug molecules to find versions with optimal therapeutic properties.

“One can use this new technology to modify a drug molecule at a late stage of synthesis, to improve the molecule’s properties without having to go back to change the synthesis from the beginning,” said study senior author Jin-Quan Yu, PhD, Frank and Bertha Hupp professor in the department of chemistry at TSRI.

The new method, reported in the journal Nature, was developed by Yu’s laboratory in collaboration with scientists at Bristol-Myers Squibb, who are already applying the method in their drug development programs.

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