Catalyst-Where-You-Want-It Method Expands the Possibilities for New Drug Development

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Newswise LA JOLLA, CANovember 10, 2014Chemists at The Scripps Research Institute (TSRI) and the Shanghai Institute of Organic Chemistry have described a method for creating and modifying organic compounds that overcomes a major limitation of previous methods. The advance opens up a large number of novel chemical structures for synthesis and evaluation, for example, as candidate pharmaceuticals.

The new method was designed to avoid an unwanted side effecta diversion of a catalyst molecule to the wrong locationthat prevents chemists from manipulating many organic compounds in the class known as heterocycles, which are commonly used as drugs.

The newly described technique gets around this obstacle by generating a reactive catalyst at precisely the desired site on a molecule to be modified.

We have already applied this technology to enable the modification of a wide range of chemical structures, including a complex drug candidate being developed by a major pharmaceutical company, said Jin-Quan Yu, professor of chemistry at TSRI.

Yu and his colleagues describe the new method in a paper published by the journal Nature on November 10, 2014.

Small Changes with Big Consequences

Heterocycles have the basic carbon-ring structures of other organic compounds, but with one or more of the carbon atoms replaced by a different atom, such as nitrogen or sulfur. Such a seemingly slight change can radically alter the properties of a compoundconferring greater solubility, for example, which is why heterocyclic structures are often preferred in modern synthetic drugs and also are found frequently in natural compounds that are used as drugs.

But heterocycles pose a particular challenge for those who would modify them. In the pharmaceutical industry, for example, chemists typically select a compound that has a desired chemical activity and then attempt to tweak it in various ways to optimize its properties and perhaps create useful new properties. The fastest way to do this is by removing a hydrogen atom from one of the compounds backbone carbon atoms and replacing it with a new functional group.

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Catalyst-Where-You-Want-It Method Expands the Possibilities for New Drug Development