Bring more good medicines faster, understand the 2021 Nobel Prize in Chemistry

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 same

Speaking 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 molecules

In 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 molecules

Before 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
.

The breakthrough research of these two scientists won them the Nobel Prize in Chemistry this year
.

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
.

The emergence of organic catalyst is like a chess piece with a brand new function on the chessboard, it has changed the rules of the entire game
.

For example, organic catalysts can continuously catalyze several chemical reactions, which greatly reduces the number of compound synthesis steps
.
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.

.
By 2011, using organic catalysis, researchers only needed 12 steps to synthesize paponylin, and the production efficiency was increased by 7000 times
.

Only 12 steps are needed to synthesize paponylin in 29 steps , and the production efficiency is 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
.
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
.

Organic catalysis makes it easier for researchers to produce curative chiral molecules, avoiding the production of mirror-symmetrical molecules.
They not only reduce production efficiency, but may also cause toxic side effects or increase the patient's metabolic burden
.

Since the beginning of this century, the application of catalysts in the chemical, pharmaceutical and other fields has developed rapidly
.
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
.
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
.

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
.

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

[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

[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://