Research could potentially add to the combined line of drugs containing the amine

chemical contact

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A research team from the University of Illinois at Urbana-Champaign has found a way to create a unique molecular structure that could open the door for new drugs to treat currently incurable diseases. .

Open a home medicine office and you may find organic derivatives of ammonia, called amines. It is one of the most fortified buildings available in medicine today. More than 40 percent of pharmaceutical and pharmaceutical candidates contain amines, and 60 percent of those amines are high -grade, so named for the three carbons fixed to a nitrogen.

Amins are found in some of the most important human medications, including antibiotics, breast cancer and leukemia medications, opioid painkillers, antihistamines, blood thinners, HIV treatments, antimigraine medications and more. They increase the solubility of the drug and can stimulate its vital functions.

Although this unique class of molecules is widespread in medicine today, most tertiary amines are not used.

This is why the traditional process of making them requires specific conditions, which are designed to limit the availability of new tertiary amines, which can treat incurable diseases. Done now.

Now, an Illinois research team led by Lycan Professor of Chemistry M. Christina White and graduate students Siraj Ali, Brenna Budaitis, and Devon Fontaine have discovered a new chemical solution, a carbon-hydrogen amination. cross-coupling reaction, to create speed. It is much easier to produce high amines without the limitations of conventional methods. Researchers believe this could be used to detect new effects with nitrogen.

This innovation in the chemist’s toolbox transforms the traditional tertiary amine building process – with its standard chemical effects requiring special conditions in each molecule – into a workable process. Held in open air and humid conditions as far as possible. for automation.

As explained by the researchers in their paper published in ScienceThis new process uses a metal catalyst known by their group (WhiteSOX / palladium) and two building blocks – major hydrocarbons (olefins based on the C – H bond) and secondary amines – to produce tertiary amino acids.

This has the potential, White explains, for chemists to take different double amines and combine them with different olefins, you can buy or sell them cheaply.

“And these are solid starters. You can get them in individual boxes, combine and compare them, and use our catalyst to make different combinations of tertiary amines,” he said. “said White. “The simplicity of this response simplifies the identification process for tertiary amino acids.”

The difference between the usual results and this new answer for making high amines is like the difference between picking a special sandwich from a menu and making your own sandwich from it. all sorts of things – the choices are much simpler.

This very simple system for the production of tertiary amines is very efficient.

“You can, in principle, run over your stove,” White explained. “You don’t have to keep it with a lot of care, you can fly in the air and you don’t have to run out of water. You just need your starters, the palladium / SOX catalyst and a little heat. should do the same as we do in the lab. “

White explained that when a pharmaceutical company wants to make high amines, they need to use special processes, but this answer allows you to take two simple, often professional ones. , start and combine them using the same process.

“Because the conditions are simple and functional for the amines and olefins there is a lot of potential to achieve this response for automation,” says White.

The main challenge overcome by the team in this finding was to solve a long -standing problem in C – H functionalization chemistry: converting a hydrogen atom into the carbon form of a molecule with a basic amine, two. work directly with amines.

Metal solvents are more likely to interact with basic amines than the C – H compounds in olefin. The team hypothesized that amino salts (amine-BF3 salts that are easy to use and maintain) could prevent this interaction with the catalyst.

As the dam changes the flow of water, the palladium / SOX catalyst regulates the slow release of amines from the salts and combines the second amine and hydrocarbon to form the amine product. tertiary.

To demonstrate the power of this new chemical solution, the researchers created 81 amines in their study, combining two complex amines, related to the treatment of the hard olefins found. the reactive process. This applies to processes that interact with secondary amines in traditional tertiary amine processing processes.

Demonstrating the potential to detect new drugs, the research team also used this new response to efficient syntheses of 12 available drug compounds, including Abilify, an anti-psychotic drug, Naftin, a anti-fungal, and 11 anti-inflammatory drugs. , including anti-depressants, Paxil and Prozac, and a blood thinner, Plavix.

In addition to this finding being used in the pharmaceutical industry as a platform to quickly identify new tertiary amino acids, the researchers believe that their catalyst-controlled slow-release design could be used. will be used by other researchers to discover many new results. nitrogen.


Amine production is maintained by the hydrogenation of amides under low conditions


More information:
Siraj Z. Ali et al, Allylic C-H amination cross-coupling supply of tertiary amines by electrophilic metal catalysis, Science (2022). DOI: 10.1126 / science.abn8382

Presented by the University of Illinois at Urbana-Champaign

Directions: Research on possible amine-containing drugs (2022, April 15) Retrieved 15 April 2022 from https://phys.org/news/2022-04-enable -line-synthesis-prevalent-amine-containing. html

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