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Controlling radicals for chemoselective synthesis of pharmaceutical ingredients

Kleij, Arjan W. (ICIQ)

Experimental Sciences & Mathematics

We developed a synthetic method for new types of pharma compounds allowing to use otherwise too reactive radical species. The process we developed is operationally simple and builds on our long-year expertise with carbon dioxide based heterocycles that are versatile precursors for many applications in fine-chemical and polymer fabrications. By using light as a source to generate radicals, we can functionalize these heterocycles and control the process from a stereo-chemistry point of view, producing thereby olefins (compounds with a C=C double bonds) that are not easy to assemble with other known approaches. Our work thus opens up new opportunities for the valorization of carbon dioxide based precursors within pharmaceutical discovery and development programs.

A photo-mediated radical approach for pharma synthons


REFERÈNCIA

Zeng Q, Nirwan Y, Benet-Buchholz J, Kleij AW 2024, 'An Expedient Radical Approach for the Decarboxylative Synthesis of Stereodefined All-Carbon Tetrasubstituted Olefins', Angewandte Chemie International Edition, 63, e202403651.
*Part of Wiley´s Hot Topics
*Highlighted by Synfacts 2024; 20 (07): 0707, DOI: 10.1055/s-0043-1773295