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2020-08-24 16:16:36

Researchers from Zelinsky Institute developed a simple method for the synthesis of previously hardly available unsymmetrically substituted N-aryl oxalamides

Oxalamides are important structural fragments of a variety of biologically active substances including natural compounds and widely used drugs. In particular, unsymmetrically substituted N-aryl oxalamides attract a great attention in scientific community as promising chelating ligands in catalysis, potential therapeutic agents, and building blocks in organic synthesis. The known methods for their preparation have a number of disadvantages, such as the need of absolute solvents, harsh reaction conditions, and a limited substrates scope.

Researchers from Laboratory № 22 of the Institute of Organic Chemistry have developed an easy synthetic route to unsymmetrically substituted N-aryl oxalamides using inexpensive and available 2,2'-biphenyldiamines, 2-chloroacetamides, sulfur, and water as starting compounds. This approach significantly expands the range of synthetically available N-aryl oxalamides with NH2 group in the side chain. The developed synthetic route will be useful in pharmacological studies and in the search for ligands for use in transition metals-catalyzed reactions.

Source:

T. A. Tikhonova, N. V. Ilment, K. A. Lyssenko, I. V. Zavarzina, Yu. A. Volkova Sulfur-mediated synthesis of unsymmetrically substituted N-aryl oxalamides by the cascade thioamidation/cyclocondensation and hydrolysis reaction Org. Biomol. Chem., 2020, 18, 5050-5060, DOI: 10.1039/D0OB00811G

 

 

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The European Academy of Sciences (Academia Europaea) was founded in 1988. It unites about four thousand globally acknowledged experts in mathematics, medicine, natural sciences, humanities, law, economy, and social and political sciences from many countries of Europe. Among its members are also European scientists who live in other regions of the world. Currently, it includes seventy two Nobel laureates and it should be highlighted that many of them were elected to the Academy before winning the Prize.
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