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Medicinal Chemistry

All articles tagged with #medicinal chemistry

New electrochemical method converts CO2 and nitrite into high-value arylglycines
science14 days ago

New electrochemical method converts CO2 and nitrite into high-value arylglycines

Researchers have developed a two-step electrochemical process to synthesize arylglycines, a class of valuable unnatural amino acids, using carbon dioxide, nitrite, and aromatic aldehydes as feedstocks. The method replaces traditional toxic reagents and harsh conditions with a Lewis acid-assisted electrocatalytic approach. Using benzaldehyde as a model substrate, the process achieved 84% conversion and 81% Faradaic efficiency for phenylglycine. The technique involves the electrochemical reduction of nitrite to hydroxylamine, which condenses with aldehydes to form oximes, followed by electroreductive carboxylation with CO2. This approach offers a sustainable alternative for producing compounds essential in medicinal chemistry and peptide natural products.

Advancements in Catalysts and Synthesis Methods for Industrial Compounds
science-and-technology3 years ago

Advancements in Catalysts and Synthesis Methods for Industrial Compounds

Researchers in China have developed a method for synthesizing a variety of methylenecyclobutane derivatives, overcoming previous challenges in regioselectivity, stereoselectivity, and functional group tolerance. The method utilizes a copper-catalyzed borylative cyclization reaction and achieves excellent yields under relatively benign reaction conditions. While the method is not enantioselective and has limitations in functional compatibility, it is considered practical and selective, opening up possibilities for the synthesis of novel and strained natural products in medicinal chemistry. The researchers aim to make the process enantioselective and expand its application to broader cyclobutane derivatives.

"Chemists Achieve 'Almost Magical' Feat: Manipulating Single Atoms within Molecules"
science-and-technology3 years ago

"Chemists Achieve 'Almost Magical' Feat: Manipulating Single Atoms within Molecules"

Chemists have developed techniques for "skeletal editing," which allows them to manipulate individual atoms within a molecule's core by deleting, adding, or swapping them. This breakthrough has the potential to revolutionize the field of organic chemistry and significantly accelerate the drug-discovery process.