Palladium(II)-Catalyzed Heck Coupling: Direct Stereoselective Synthesis of -Aryl Glycosides from Nonactivated Glycals and Thianthrenium Salts.

Here, we report an efficient Pd(II)-catalyzed Heck coupling reaction utilizing modular and readily available thianthrenium salts. The tunability and ease of thianthrenium salts facilitated the integration of glycals with drugs, natural products, and peptides. This method allows the incorporation of diverse glycals into structurally varied aglycon components without directing groups or prefunctionalization and provides a practical method for synthesizing -aryl glycosides, offering a new avenue for the production of complex glycosides with potential applications.

Direct Construction of C-Alkyl Glycosides from Non-Activated Olefins via Nickel-Catalyzed C(sp)─C(sp) Coupling Reaction.

Among C-glycosides, C-alkyl glycosides are significant building blocks for natural products and glycopeptides. However, research on efficient construction methods for C-alkyl glycosides remains relatively limited. Compared with Michael acceptors, non-activated olefins are more challenging substrates and have rarely been employed in the construction of C-glycosides.

Cobalt(II)-Catalyzed C(sp )-C(sp ) Coupling for the Direct Stereoselective Synthesis of 2-Deoxy-C-Glycosides from Glycals.

We report a ligand-controlled Co -catalyzed C(sp )-C(sp ) coupling hydroalkylation for direct and β-selective synthesis of 2-deoxy-C-glycosides from glycals. This reaction proceeds by a radical pathway for alkyl halide activation and is β-selective through ligand control. This approach may inspire the development of further stereoselective coupling reactions with potential application in the field of carbohydrates.

Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.

CDK9 is an essential drug target correlated to the development of acute myeloid leukemia (AML). Starting from the hit compound , which was discovered through a screening of our in-house compound library, the structural modifications were carried out based on the bioisosterism and scaffold hopping strategies. Consequently, compound displayed the optimal CDK9 inhibitory activity with an IC value of 5.