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 Discovery of a Key Regulatory Gene in Cardiac Valve Formation
24.05.2017 | Universität Basel

nachricht Carcinogenic soot particles from GDI engines
24.05.2017 | Empa - Eidgenössische Materialprüfungs- und Forschungsanstalt

All articles from Life Sciences >>>

The most recent press releases about innovation >>>

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

Im Focus: A quantum walk of photons

Physicists from the University of Würzburg are capable of generating identical looking single light particles at the push of a button. Two new studies now demonstrate the potential this method holds.

The quantum computer has fuelled the imagination of scientists for decades: It is based on fundamentally different phenomena than a conventional computer....

Im Focus: Turmoil in sluggish electrons’ existence

An international team of physicists has monitored the scattering behaviour of electrons in a non-conducting material in real-time. Their insights could be beneficial for radiotherapy.

We can refer to electrons in non-conducting materials as ‘sluggish’. Typically, they remain fixed in a location, deep inside an atomic composite. It is hence...

Im Focus: Wafer-thin Magnetic Materials Developed for Future Quantum Technologies

Two-dimensional magnetic structures are regarded as a promising material for new types of data storage, since the magnetic properties of individual molecular building blocks can be investigated and modified. For the first time, researchers have now produced a wafer-thin ferrimagnet, in which molecules with different magnetic centers arrange themselves on a gold surface to form a checkerboard pattern. Scientists at the Swiss Nanoscience Institute at the University of Basel and the Paul Scherrer Institute published their findings in the journal Nature Communications.

Ferrimagnets are composed of two centers which are magnetized at different strengths and point in opposing directions. Two-dimensional, quasi-flat ferrimagnets...

Im Focus: World's thinnest hologram paves path to new 3-D world

Nano-hologram paves way for integration of 3-D holography into everyday electronics

An Australian-Chinese research team has created the world's thinnest hologram, paving the way towards the integration of 3D holography into everyday...

Im Focus: Using graphene to create quantum bits

In the race to produce a quantum computer, a number of projects are seeking a way to create quantum bits -- or qubits -- that are stable, meaning they are not much affected by changes in their environment. This normally needs highly nonlinear non-dissipative elements capable of functioning at very low temperatures.

In pursuit of this goal, researchers at EPFL's Laboratory of Photonics and Quantum Measurements LPQM (STI/SB), have investigated a nonlinear graphene-based...

All Focus news of the innovation-report >>>

Anzeige

Anzeige

Event News

Marine Conservation: IASS Contributes to UN Ocean Conference in New York on 5-9 June

24.05.2017 | Event News

AWK Aachen Machine Tool Colloquium 2017: Internet of Production for Agile Enterprises

23.05.2017 | Event News

Dortmund MST Conference presents Individualized Healthcare Solutions with micro and nanotechnology

22.05.2017 | Event News

 
Latest News

Physicists discover mechanism behind granular capillary effect

24.05.2017 | Physics and Astronomy

Measured for the first time: Direction of light waves changed by quantum effect

24.05.2017 | Physics and Astronomy

Marine Conservation: IASS Contributes to UN Ocean Conference in New York on 5-9 June

24.05.2017 | Event News

VideoLinks
B2B-VideoLinks
More VideoLinks >>>