Like human hands, many molecules that make up drugs come in two shapes, right and left. But usually only one of the two versions has the desired effect; the other is at best useless and sometimes even harmful. For example, side effects from the morning sickness drug Thalidomide resulted in profound birth defects because one shape of the molecule was therapeutic and the other was dangerous.
Don Coltart, an assistant professor of chemistry at Duke, appears to have found a way to make synthetic ketone molecules in just one version or the other using a process that is faster, cheaper and less wasteful than the best techniques now available.
And unlike previous attempts to make just one shape of these molecules, a process called asymmetric synthesis, the new method should be able to scaling up to industrial manufacturing quantities.
"Asymmetric synthesis of ketones is not new, but we can do it more practically and easily," said Coltart, who developed the new technique with graduate student Daniel Lim."
Though well-known to the pharmaceutical industry, this problem of molecular handedness in ketones has been difficult to solve. Academic labs have succeeded at asymmetric synthesis over the last two decades, but only by using extreme conditions (e.g. temperatures of -100 degrees Celsius), and costly and time-consuming steps.
Conducted at zero C to -40 C, the new process uses a small molecule called a "chiral auxiliary" to attach pieces to a molecule being built, which causes the new pieces to have the correct handedness. The process is up to 98 percent accurate, Coltart said, and the auxiliary molecules can be easily released and recycled after they've done their work.
"He did something very different," said Samuel Danishefsky of Columbia University and the Memorial Sloan-Kettering Cancer Center, who is Coltart's former post-doctoral mentor. "You could have had a hundred people look at this problem and not see it the way he did. It's a very nice idea."
Coltart said there is a huge need for drug companies to be more selective to make better drugs with fewer side effects, which this new process might help achieve. Pharmaceutical companies might also use the new technique to turn existing formulations of drugs sold as mixtures into a pure form having only the active form of the drug, giving them another seven years of patent protection.
Karl Leif Bates | EurekAlert!
Coat of proteins makes viruses more infectious and links them to Alzheimer's disease
27.05.2019 | Stockholm University
The Secret of the Rock Drawings
24.05.2019 | Max-Planck-Institut für Chemie
Researchers from Sweden's Chalmers University of Technology and the University of Gothenburg present a new method which can double the energy of a proton beam produced by laser-based particle accelerators. The breakthrough could lead to more compact, cheaper equipment that could be useful for many applications, including proton therapy.
Proton therapy involves firing a beam of accelerated protons at cancerous tumours, killing them through irradiation. But the equipment needed is so large and...
A new assessment of NASA's record of global temperatures revealed that the agency's estimate of Earth's long-term temperature rise in recent decades is accurate to within less than a tenth of a degree Fahrenheit, providing confidence that past and future research is correctly capturing rising surface temperatures.
The most complete assessment ever of statistical uncertainty within the GISS Surface Temperature Analysis (GISTEMP) data product shows that the annual values...
Physicists at the University of Basel are able to show for the first time how a single electron looks in an artificial atom. A newly developed method enables them to show the probability of an electron being present in a space. This allows improved control of electron spins, which could serve as the smallest information unit in a future quantum computer. The experiments were published in Physical Review Letters and the related theory in Physical Review B.
The spin of an electron is a promising candidate for use as the smallest information unit (qubit) of a quantum computer. Controlling and switching this spin or...
Engineers at the University of Tokyo continually pioneer new ways to improve battery technology. Professor Atsuo Yamada and his team recently developed a...
With a quantum coprocessor in the cloud, physicists from Innsbruck, Austria, open the door to the simulation of previously unsolvable problems in chemistry, materials research or high-energy physics. The research groups led by Rainer Blatt and Peter Zoller report in the journal Nature how they simulated particle physics phenomena on 20 quantum bits and how the quantum simulator self-verified the result for the first time.
Many scientists are currently working on investigating how quantum advantage can be exploited on hardware already available today. Three years ago, physicists...
29.04.2019 | Event News
17.04.2019 | Event News
15.04.2019 | Event News
27.05.2019 | Information Technology
27.05.2019 | Physics and Astronomy
27.05.2019 | Life Sciences