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New chemistry technique simplifies drug-making

"This new process provides an entirely new pathway for constructing one of the 'cornerstones' of chiral molecules," said researcher Jin-Quan Yu.

By Brooks Hays
Researchers have come up with a faster, easier way to make medical compounds. Photo by VonaUA/Shutterstock
A team of researchers in China and the United States have found an easier way to turn chemicals into drugs.
One of the most difficult parts of drug synthesis is creating "one-handed" molecules. Most medical compounds involve chiral molecules, molecules that can exist in two forms -- as two mirror images, like a right hand and left hand.
Often, the mirror image of a medically beneficial chiral molecule can have adverse effects. But producing only the wanted form of a chiral molecule isn't easy.
The latest research simplifies the process.
Many drugs are built on beta-chiral centers. Beta-chiral centers are made by taking a beta methylene molecule -- a molecule with a carbon atom attached to two hydrogen atoms by single bonds -- and replacing one of the two hydrogen atoms with a new group of atoms, called a functional group.
The current method for this process is called conjugate addition, which requires the creation of a double bond between the carbon and functional group atoms.
Scientists have come up with a new way to break and replace the carbon-hydrogen bond using a palladium atom. The method offers a shortcut and reduces waste while ensuring proper chirality. The catalyst is much more precise in breaking the exact carbon-hydrogen bond.
"It is important to be able to synthesize only one of two mirror images of the molecule, and development of new catalytic methods that achieve this goal, starting with carbon-hydrogen bonds, is highly desired," Guosheng Liu, lead researcher and a professor at the Shanghai Institute of Organic Chemistry, explained in a news release.
The researchers shared their breakthrough in a new paper published in the journal Science.
"This new process provides an entirely new pathway for constructing one of the 'cornerstones' of chiral molecules, namely, beta-chiral centers, and should accelerate the development of chiral drugs," concluded Jin-Quan Yu, a professor of chemistry at the Scripps Research Institute.

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