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Scripps Research Institute scientists find easier way to make new drug compounds
Date:6/27/2012

LA JOLLA, CA Scientists at The Scripps Research Institute have developed a powerful new technique for manipulating the building-block molecules of organic chemistry. The technique enables chemists to add new functional molecules to previously hard-to-reach positions on existing compoundsmaking it easier for them to generate new drugs and other organic chemicals.

"This is a basic tool for making novel chemical compounds, and it should have a wide range of applications," said Jin-Quan Yu, PhD, a professor at Scripps Research and senior author of the new report, published in the June 28, 2012 issue of the journal Nature. The co-lead authors are Dasheng Leow, PhD, a former Yu lab member who is now a researcher at the A*Star Institute of Bioengineering and Nanotechnology in Singapore, and Gang Li, PhD, a postdoctoral fellow in the Yu laboratory.

"Controlled selectivity and reaction efficiency are important goals in synthetic chemistry methods for discovering and manufacturing therapeutic and diagnostic agents," said Robert Lees, PhD, who oversees chemical synthesis grants at the National Institutes of Health's National Institute of General Medical Sciences, which partially supported the work. "Professor Yu's work is an exciting example of progress toward those goals, and his novel methods are likely to find broad utility in pharmaceutical research."

The new advance is a method for "CH activation"chemists' code for the removal of a simple hydrogen atom from the carbon backbone of an organic molecule, and the replacement of that hydrogen atom with a functional chemical group. Compared to the traditional method, in which chemists modify only the existing functional groups on a compound, CH activation more directly boosts the complexity of a compound, giving it potentially valuable new properties.

Overcoming Technical Obstacles

Over the past decade, Yu has helped to pioneer the development of versatile CH-
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Contact: Mika Ono
mikaono@scripps.edu
858-784-2052
Scripps Research Institute
Source:Eurekalert  

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