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In 2021, the Nobel Prize in Chemistry was awarded to two pioneers in the field of "asymmetric organic catalysis"
The new chemical synthesis tools brought by these two scientists have extremely important application value in the development and manufacture of new drugs, bringing tangible changes to patients around the world
Look the same, but not the same
Look the same, but not the sameSpeaking of "asymmetric catalysis", we must first start with chiral molecules.
Although chiral molecules have exactly the same molecular formula, like our left hand and right hand, the three-dimensional structure is mirror image symmetry, just the opposite
Image source: !Original:UnknownVector: - πϵρήλιο, Public domain, via Wikimedia Commons
Previous studies have long found that the human body’s response to chiral molecules can be quite different .
The human body's response to chiral molecules can be very different
▲Different chiral structures of limonene make us smell different (picture source: reference [3])
▲Different chiral structures of limonene make us smell different (picture source: reference [3])In the treatment of diseases, this structural difference can turn a drug from a good medicine into a poison
This structural difference can change a drug from a good medicine to a poison
Catalysts-the key to producing chiral molecules
Catalysts-the key to producing chiral moleculesIn the chemical reaction that produces the compound, the catalyst has an important function
Many proteases are characterized by only catalyzing the formation of compounds with a chiral configuration
Chemists William S.
Image source: The Nobel Prize in Chemistry 2001.
This breakthrough brought about the first industrial-scale "asymmetric catalysis" synthesis, and the resulting drug is levodopa (L-DOPA) for the treatment of Parkinson's disease
New tools for building molecules
New tools for building moleculesBefore 2000, there were two types of catalysts: metal or protease
There are two types of catalysts: metal or protease
Another type of catalyst is proteases, which are very effective "asymmetric catalysts", and they are also objects that scientists want to imitate
Although protease is composed of hundreds of amino acids, it is only one or a few of them that really drive the catalytic effect
▲Dr.
▲Dr.
At the same time, Professor David MacMillan at the University of California at Berkeley was also working towards the same goal
Professor MacMillan named this catalytic reaction "organocatalysis".
We introduce a new organic catalysis strategy, which is expected to be used in a series of asymmetric transformations in the future
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The breakthrough research of these two scientists won them the Nobel Prize in Chemistry this year
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Make drug production faster and easier
Make drug production faster and easier Nobel Prize Committee member Peter Somfai said after the announcement of the chemistry prize that the appearance of organic catalyst is like a chess piece with a brand new function on the chessboard, which has changed the rules of the entire game
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.
For example, organic catalysts can continuously catalyze several chemical reactions, which greatly reduces the number of compound synthesis steps
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Taking the very complex natural molecule paponylin as an example, when it was first synthesized in 1952, it required 29 different chemical reactions, and only 0.
0009% of the raw materials eventually formed paponylin, and the rest was wasted in the reaction process.
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By 2011, using organic catalysis, researchers only needed 12 steps to synthesize paponylin, and the production efficiency was increased by 7000 times
.
.
Image source: 123RF
In terms of drug production, organic catalysis allows researchers to more easily produce curative chiral molecules and avoid the production of mirror-symmetric molecules.
They not only reduce production efficiency, but may also cause toxic side effects or increase the metabolic burden of patients
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A large number of biomedical companies are already using this technology to simplify the production process of drugs, including paroxetine for the treatment of anxiety and depression, and the antiviral drug oseltamivir for the treatment of respiratory infections
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They not only reduce production efficiency, but may also cause toxic side effects or increase the patient's metabolic burden
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Since the beginning of this century, the application of catalysts in the chemical, pharmaceutical and other fields has developed rapidly
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In order to meet the synthesis process of different drug molecules, the catalytic platforms using metals, biological enzymes, and small organic molecules have their respective strengths and brought a variety of innovative drugs to patients around the world
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For example , Hequan Pharmaceutical, a subsidiary of WuXi AppTec, has developed green, efficient and safe synthetic processes for a variety of innovative drugs for more than ten years
.
These are typical cases where science is transformed into practical applications to benefit mankind
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These are typical cases where science is transformed into practical applications to benefit mankind
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We congratulate the two scientists who won the Nobel Prize again, and we look forward to more scientific innovations that can help the research and development of new drugs, bring more good drugs and new drugs to the world, and improve health
.
Reference materials:
Reference materials: [1] The Nobel Prize in Chemistry 2021.
Retrieved October 6.
2021.
from https:// The Nobel Prize in Chemistry 2021.
Retrieved October 6.
2021.
from https:// [2] Pioneers of asymmetric organocatalysis win 2021 Nobel Prize in Chemistry.
Retrieved October 6.
2021.
from https://cen.
acs.
org/people/nobel-prize/Asymmetric-organocatalysis-List-MacMillan-Nobel-Prize-Chemistry -organic-synthesis/99/web/2021/10
Retrieved October 6.
2021.
from https://cen.
acs.
org/people/nobel-prize/Asymmetric-organocatalysis-List-MacMillan-Nobel-Prize-Chemistry -organic-synthesis/99/web/2021/10
[3] Their tools revolutionised the construction of molecules.
Retrieved October 6.
2021.
from https:// Their tools revolutionised the construction of molecules.
Retrieved October 6.
2021.
from https:// [4] The Nobel Prize in Chemistry 2001.
Retrieved October 6.
2021.
from https:// The Nobel Prize in Chemistry 2001.
Retrieved October 6.
2021.
from https:// [5] Catalytic asymmetric synthesis.
Retrieved October 6.
2021.
from https:// Catalytic asymmetric synthesis.
Retrieved October 6.
2021.
from https://