Oxidant-Free Arene-Azole Cross-Coupling via Acridinium Salts
9-Mesityl-10-methylacridinium perchlorate [M1774] is utilized as a photocatalyst in a highly effective and mild C-N cross coupling transformation between alkylated arenes and azoles that is both photocatalyzed and oxidant free. Cross-coupling methods between nitrogen arenes and aromatic moieties are essential for the production of key pharmaceutical compounds. Here regioselective and oxidant-free C-N cross-couplings are required, particularly due to methylarenes’ sensitivity to exudative conditions. Additionally, the only waste product produced is a gaseous hydrogen with the reaction requiring no oxidant and is regioselective to a variety of aromatic moieties.
Building Blocks for Bioisosteric Replacement in Medicinal Chemistry
Cross-coupling reactions have become ubiquitous in organic synthesis and are essential for the expansion of building block libraries. However, it has been speculated that the planarity of compounds would cause unpredictable and undesirable bioavailability and toxicity owing their deficiencies to insolubility. O0466 and B5032 are bioisosteres of morpholine and piperazine respectively. B5479, M3149, and D5542 are bioisosteres of benzene rings. These building blocks are expected to assist in introducing more sp3 carbon character to drug candidates, leading to improved solubility and increasing 3-dimensionality.
Released in August, TCI's latest issue features Victor R. de la Rosa and Richard Hoogenboom's article on biocompatible polymers called "Poly(2-oxazoline)s: The Versatile Polymer Platform". We also feature research on:
Boronic acid derivatives are crucial reactants for the Suzuki-Miyaura cross-coupling reaction. TCI has 3 newly released boronic acid derivatives for your research with products such as boronic acids, boronate esters, and trifluoroborate salts also available.
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