A series of 1,10-phenanthroline derivatives bearing multi(aryl)methyl substituents was synthesized and applied to the Ir-catalyzed C(sp3)–H borylation of alkanes using HBpin. Some Ir complexes bearing the developed 1,10-phenanthroline ligands exhibited superior catalytic activity compared with those containing conventional 1,10-phenanthroline ligands, such as 3,4,7,8-tetramethyl-1,10-phenanthroline and 2-methyl-1,10-phenanthroline. These studies revealed that 3,8-multi(aryl)methyl-substituted 1,10-phenanthrolines are crucial for catalytic activity, and that the steric bulk of the multi(aryl)methyl groups significantly influences the catalytic performance.

A convenient stereoselective organocatalytic disulfonylation of epoxides was developed. This reaction uses various sulfonic anhydrides, such as methanesulfonic anhydride or p-toluenesulfonic anhydride, and is catalyzed with pyridine N-oxide derivatives. Washing the sulfonic anhydrides with Et2O was key to the success of the reaction. Several disulfonylated vicinal diols were obtained in high yield. The reaction was also applied to 1,2-disubstituted epoxides to provide anti-disulfonylated vicinal diols in high yield.

A synthetic study on the formation of the main tetracyclic core of myrioneurinol, an antiplasmodial compound belonging to the myrioneuron alkaloid family, has been completed. This approach begins with a tetralone derivative and emphasizes an oxidative dearomatizing 1,3-alkyl shift process mediated by an environmental-friendly hypervalent iodine reagent as a pivotal step. Other steps include formylation, an SN2-Michael cascade process, oxidative acetalization, and trans-acetalization. To prove the concept of a viable strategy, the key tetracyclic system obtained was transformed into a known myrioneurinol intermediate observed during the synthesis of Prof. Ma and coworkers in 2022. Moreover, this study identified a variety of complex and intriguing polycyclic systems as by-products, demonstrating the synthetic potential of this approach in the rapid formation of compact, functionalized scaffolds.

A general approach was developed to the synthesis of 3-amino-4-arylquinolin-2(1H)-ones and 3-amino-4-arylquinoline-2(1H)-thiones, based on simple and readily available reagents, with good overall yields of up to 76%. A broad variety of aryl and heteroaryl substituents introduced at the C-4 position of the quinoline system was achieved. The route can also be used for the synthesis of 4-alkyl derivatives, as shown in the example of 4-methylquinolines. Solutions of some synthesized compounds emit in the blue-violet region of the visible spectrum with fluorescence quantum yields of up to 0.33 upon UV irradiation.

We report the synthesis of an azide-bearing L-3,4dihydroxyphenylalanine derivative, AZ-DOPA, as a versatile building block for constructing antifouling interfaces via click chemistry. AZ-DOPA was synthesized through a sequence of protecting-group manipulations and azidation. By exploiting the material-independent adhesive nature of melanin-like species, stable azide-functionalized coatings were formed on various substrates. The resulting surfaces served as reactive platforms for the immobilization of a propargyl-based zwitterion (PBZ) via copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC). The PBZ-modified surfaces exhibited excellent antifouling performance, achieving a 95.7% reduction in bacterial adhesion. This work demonstrates that the combination of AZ-DOPA-based coatings and zwitterionic functionalization provides a robust and universal strategy for the development of highly effective antifouling surfaces.

Abstract A novel 3D-printed platform for photochemical reaction miniaturization has been designed, created, and characterized to expedite photoredox reaction optimization. The system offers two configurations, supporting throughput of 16 or 96 parallel experiments. This approach provides a cost-effective and sustainable strategy to access large datasets with minimal economic burden, allowing its implementation in virtually all research groups interested in photochemistry. Initial characterization data for both configurations and blueprints of the 3D-printed device are provided to ensure rapid and straightforward implementation.

Abstract A liquid–liquid extraction process was developed to isolate a macrocyclic peptide product generated via biocatalysis in the synthesis of enlicitide decanoate. Applying traditional purification methods for enzymatic cascades is challenging due to the presence of proteins, salts, and organic impurities that complicate downstream processing. To address this complexity, we employed a vision-guided, automated, high-throughput screening platform that enabled the systematic evaluation of hundreds of process conditions. Through comprehensive screening, we successfully identified optimal conditions for the selective isolation of the macrocyclic peptide product, achieving 93% recovery with no detectable protein residue. This approach served to streamline purification and enhanced overall process efficiency, demonstrating the utility of automated high-throughput screening for addressing complex purification challenges in biocatalytic process development.

Abstract This works reports an efficient and general method for synthesizing β-ketophosphonate derivatives using AgNO3 as the catalyst and K2S2O8 as the oxidant under mild conditions (room temperature and open-air atmosphere). The procedure is effective under simple and very convenient conditions with easy isolation and purification of the product. Potassium persulfate (K2S2O8) has emerged as a cost-effective, easily accessible inorganic oxidant. K2S2O8 exhibited a unique utility as the most efficient oxidant due to its greater solubility in organic media. A broad substrate scope and suitable functional group compatibility were observed. Experimental studies show that the reaction undergoes a radical process.

Abstract Herein we provide a bismuth-catalyzed reduction of nitroarenes to anilines using a simple and air-stable bismuth pre-catalyst. The reaction uses up to 5 mol% of Bi catalyst and PhSiH3 as the terminal reductant under mild conditions. The Bi pre-catalyst is an air-stable Bi(III), which is converted in the catalytically active species in situ by the PhSiH3. The mild reducing conditions permit the presence of aromatic halides. In analogy to the previous processes in bismuth catalysis, the reaction is speculated to proceed through a low-valent Bi(I)/Bi(III) redox cycle.

Levulinic acid (LA) is a key biomass-derived platform molecule that provides access to a wide range of value-added chemicals through selective functional group manipulation. Although transition-metal catalysis has traditionally dominated LA upgrading, recent years have witnessed rapid progress in transition-metal-free synthetic strategies based on main-group reagents, Brønsted (or Lewis) acids and bases, and organocatalytic activation modes. This Short Review summarizes recent advances in the metal-free synthesis and transformation of levulinic acid, with a particular focus on reaction design and mechanistic features relevant to organic synthesis. Key topics include chemoselective reduction to γ-valerolactone and related oxygenates, pH-controlled oxidative C–C bond cleavage to functional organic acids, acid-mediated condensation reactions toward polymer-relevant monomers, and metal-free amination and cyclization pathways affording nitrogen-containing heterocycles. By organizing these transformations according to reaction class and selectivity control, this review highlights how foundational organic reactivity can be leveraged to achieve efficient and sustainable valorization of levulinic acid without reliance on transition metals.