New Insights in Coupling Reactions

Dear Colleagues,

The transition metal-catalyzed cross-coupling strategy established in 20th century has become an important tool to create a carbon–carbon bond for the target molecules, which now encompass a range of aryl, alkynyl, and alkenyl substrates as counterpart of organometallic nucleophiles. These cross-coupling methods are known to be particularly useful for both laboratorial and industrial synthesis of building blocks for biologically active compounds and organic materials. Aiming at further advances and application of cross-coupling synthesis, new research on academic and industrial developments has appeared on a regular basis.

The classical cross-coupling strategy would rely on the use of aryl halides (X = I, Br, Cl) and aryl metallic compounds (e.g., [M] = [Zn]: Negishi, [B]: Suzuki-Miyaura, [Sn]: Stille) in employing transition metal catalysts, such as palladium complex, while inspired by the concept of green and sustainable chemistry, more direct C–H functionalization using organic halides or organometallic compounds as one of these coupling partner was suggested in the past decade. Furthermore, through the success of controlling the oxidative cross-coupling selectivities, the most ideal synthetic route in view of the green chemistry that directly uses two molecules of C–H groups for a new bond-forming event has been realized in recent years, even for sp3 C–H bonds.

This Special Issue aim to highlight recent trends and new insights in advancing cross-couplings with estimating their continuous developments in future. The guest editors welcome review and original research articles associated with recent achievements in this area, regarding catalysts, substrates, reaction systems, etc. Areas to be covered in this Special Issue may include but are not limited to the extension of the known synthetic strategy and application to the useful organic compounds, i.e., bioactive molecules and organic materials. Indeed, promising new synthetic applications targeting the very difficult functionalizations of aqueous biological macromolecules, such as peptides and DNAs, have been found in recent drug discovery studies.

As guest editors, we hope that this Special Issue will inspire authors and readers as much as the researchers engaged in this area.

Prof. Dr. Toshifumi Dohi
Prof. Dr. Gianfranco Favi
Guest Editors

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• coupling
• catalysts
• C–X and hetero-X functionalizations
• C–H activations
• C–H functionalizations
• organic materials
• pharmaceutical compounds
• heterocycles
• heteroaromatic compounds
• biological molecules