Forum for Science, Industry and Business

Sponsored by:     3M 
Search our Site:

 

New chemical synthesis could streamline drug design

17.08.2009
New method gives drug designers more flexibility

A team of MIT chemists has devised a new way to add fluorine to a variety of compounds used in many drugs and agricultural chemicals, an advance that could offer more flexibility and potential cost-savings in designing new drugs.

Drug developers commonly add fluorine atoms to drugs, such as the cholesterol-lowering rosuvastatin, to keep the body from breaking them down too quickly. Many of these drugs contain aromatic rings — a type of six-carbon ring — and attaching a fluorine atom to the rings can be a difficult, expensive process.

"It's hard to add fluorine at a late stage, once you have a complete molecule already put together, because traditional methods can be quite harsh with respect to temperature or other factors," says Stephen L. Buchwald, the Camille Dreyfus Professor of Chemistry at MIT.

In their new technique, Buchwald and his colleagues used a palladium catalyst to attach a fluorine atom to aromatic compounds. The technique could be used in the design and testing of new drugs, or to create new imaging agents for positron emission tomography (PET) scanning.

Donald Watson, a former postdoctoral associate in Buchwald's lab, now an assistant professor of chemistry at the University of Delaware, is lead author of a paper describing the new synthesis in the Aug. 13 early online edition of Science.

During the new process, the palladium catalyst removes a group of atoms called a triflate attached to the aromatic compound, then replaces it with a fluorine atom taken from a simple salt, such as cesium fluoride. This marks the first time chemists have replaced a triflate attached to an aromatic ring with a fluorine atom in one catalytic reaction.

"Many people believed it would not be possible to do this," says Buchwald.

"While the method is probably not currently efficient enough to be used in manufacturing, we are working to speed up the reaction, increase its efficiency and make it more environmentally and user-friendly," says Buchwald. "We ultimately hope to make it general enough to be useful for manufacturing."

The research was funded by the National Institutes of Health. Other authors of the paper are visiting student Mingjuan Su and chemistry graduate student Georgiy Teverovskiy, and postdoctoral fellows Yong Zhang, Jorgé García-Fortanet

Jen Hirsch | EurekAlert!
Further information:
http://www.mit.edu

More articles from Life Sciences:

nachricht New risk factors for anxiety disorders
24.02.2017 | Julius-Maximilians-Universität Würzburg

nachricht Stingless bees have their nests protected by soldiers
24.02.2017 | Johannes Gutenberg-Universität Mainz

All articles from Life Sciences >>>

The most recent press releases about innovation >>>

Die letzten 5 Focus-News des innovations-reports im Überblick:

Im Focus: Breakthrough with a chain of gold atoms

In the field of nanoscience, an international team of physicists with participants from Konstanz has achieved a breakthrough in understanding heat transport

In the field of nanoscience, an international team of physicists with participants from Konstanz has achieved a breakthrough in understanding heat transport

Im Focus: DNA repair: a new letter in the cell alphabet

Results reveal how discoveries may be hidden in scientific “blind spots”

Cells need to repair damaged DNA in our genes to prevent the development of cancer and other diseases. Our cells therefore activate and send “repair-proteins”...

Im Focus: Dresdner scientists print tomorrow’s world

The Fraunhofer IWS Dresden and Technische Universität Dresden inaugurated their jointly operated Center for Additive Manufacturing Dresden (AMCD) with a festive ceremony on February 7, 2017. Scientists from various disciplines perform research on materials, additive manufacturing processes and innovative technologies, which build up components in a layer by layer process. This technology opens up new horizons for component design and combinations of functions. For example during fabrication, electrical conductors and sensors are already able to be additively manufactured into components. They provide information about stress conditions of a product during operation.

The 3D-printing technology, or additive manufacturing as it is often called, has long made the step out of scientific research laboratories into industrial...

Im Focus: Mimicking nature's cellular architectures via 3-D printing

Research offers new level of control over the structure of 3-D printed materials

Nature does amazing things with limited design materials. Grass, for example, can support its own weight, resist strong wind loads, and recover after being...

Im Focus: Three Magnetic States for Each Hole

Nanometer-scale magnetic perforated grids could create new possibilities for computing. Together with international colleagues, scientists from the Helmholtz Zentrum Dresden-Rossendorf (HZDR) have shown how a cobalt grid can be reliably programmed at room temperature. In addition they discovered that for every hole ("antidot") three magnetic states can be configured. The results have been published in the journal "Scientific Reports".

Physicist Dr. Rantej Bali from the HZDR, together with scientists from Singapore and Australia, designed a special grid structure in a thin layer of cobalt in...

All Focus news of the innovation-report >>>

Anzeige

Anzeige

Event News

Booth and panel discussion – The Lindau Nobel Laureate Meetings at the AAAS 2017 Annual Meeting

13.02.2017 | Event News

Complex Loading versus Hidden Reserves

10.02.2017 | Event News

International Conference on Crystal Growth in Freiburg

09.02.2017 | Event News

 
Latest News

Stingless bees have their nests protected by soldiers

24.02.2017 | Life Sciences

New risk factors for anxiety disorders

24.02.2017 | Life Sciences

MWC 2017: 5G Capital Berlin

24.02.2017 | Trade Fair News

VideoLinks
B2B-VideoLinks
More VideoLinks >>>