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Fluorine-based novel drug synthesis at lightning pace

Fluorine-based new drug synthesis at lightning speed
Analysis Picture. Credit score: POSTECH

How quick is one second? The length of a second will be outlined as one 86,four-hundredth of a 24-hour day. A bullet practice touring at 300 km per hour can cowl a distance of 83 meters in a single second. On common, a person’s blink lasts for 0.3 seconds, permitting for 3 blinks to happen inside one second. A joint crew of researchers from POSTECH has proposed a synthesis technique for fluorine-based compound by way of a fast mixing response between a gaseous element and liquid that takes lower than a single second.

The analysis crew led by Professor Dong-Pyo Kim and Jeong-Un Joo (Division of Chemical Engineering at POSTECH), and Professor Heejin Kim and Hyune-Jea Lee (at the moment, a researcher at Samsung Superior Institute of Know-how) from the Division of Chemistry at Korea College has efficiently developed a brand new technique for synthesizing trifluoromethyl intermediate (-CF3) from fluoroform (CHF3).

It entails the usage of a particular reactor able to reaching an ultra-fast mixing between gasoline and liquid. This technique provides promising prospects for the synthesis of novel fluorine-based new medicine. The analysis was printed in Nature Communications.

Fluorine isn’t present in its pure type naturally, however as a substitute exists solely within the type of numerous chemical compounds. Sodium fluoride, a compound containing fluorine, is used as an ingredient in toothpaste attributable to its capacity to coat enamel and forestall cavities.

Latest research have highlighted the potential of artificial drug molecules containing fluorine as they possess excessive permeability into cell membranes of diseased tissues and exhibit robust binding affinity in opposition to proteins. Consequently, there’s rising curiosity within the improvement of medicine containing fluorine.

There are a number of approaches to synthesizing trifluoromethyl, however probably the most cost-effective technique entails substituting a hydrogen atom from fluoroform, a easy precursor, with one other factor or practical group. Nonetheless, gaseous fluoroform is risky, which makes it tough to combine with liquids and reveals low reactivity. Furthermore, it decomposes immediately, requiring the addition of a substance that may react with it. Sadly, this course of may end up in unintended chemical reactions that result in a low yield of trifluoromethyl.

To deal with the problem of synthesizing trifluoromethyl from fluoroform, the analysis crew developed a novel gas-liquid reactor with a zigzag-shaped channel and extremely permeable non-porous membranes sandwiched between higher and decrease channels. This configuration allowed for the swirling and mixing of superbase, a liquid utilized for dehydrogenation, and gaseous fluoroform throughout the reactor.

By breaking fluoroform bubbles into smaller items to extend the contact space between gasoline and liquid, the crew was in a position to successfully produce trifluoromethyl anion (CF3). Not like conventional approaches, they produced a fluoride intermediate successfully with out requiring stabilizers or components.

The analysis crew synthesized a fluorine-based compound by instantly including a compound that may react with the fluoride anion intermediate. Your entire course of, which concerned the technology of a fluorine anion intermediate from fluoroform came about inside a second. The crew maximized the formation of a trifluoromethyl anion, which is thought to be short-lived, and quickly facilitated the following response earlier than the intermediate decomposed.

This technique allowed for improved yield of fluoride-based compounds and launched a strong approach for the synthesis of fluorine-based medicine.

The analysis findings have vital implications for industrial functions within the economically environment friendly synthesis of fluoride compounds, making them extra sensible as effectively contributing considerably to research on a number of unstable intermediates.

Extra info:
Hyune-Jea Lee et al, Ex-situ technology and artificial utilization of naked trifluoromethyl anion in movement by way of fast biphasic mixing, Nature Communications (2023). DOI: 10.1038/s41467-022-35611-9

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Pohang College of Science and Know-how

Fluorine-based novel drug synthesis at lightning pace (2023, Might 22)
retrieved 22 Might 2023

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