Palladium-Catalyzed <i>ortho</i>–C‑H Arylation of Acetophenone Oxime Ethers with Aryl Pinacol Boronic Esters

We report an efficient palladium-catalyzed <i>ortho</i>–C-H arylation of acetophenone oxime ethers with aryl pinacol boronic esters, leading to the synthesis of biaryl derivatives in good yields. Sequential process of iridium-catalyzed C–H borylation and palladium-catalyzed <i>ortho</i>–C-H arylation directed to access functionalized arenes

Synthesis of Aryl Thioethers through the <i>N</i>‑Chlorosuccinimide-Promoted Cross-Coupling Reaction of Thiols with Grignard Reagents

A convenient one-pot approach for the synthesis of aryl sulfides through the coupling of thiols with Grignard reagents in the presence of <i>N</i>-chlorosuccinimide is described. The sulfenylchlorides were formed when thiols were treated with <i>N</i>-chlorosuccinimide, and the resulting sulfenylchlorides were then directly reacted with Grignard reagents to provide aryl sulfides in good to excellent yields under mild reaction conditions. Functional groups including ester, fluoro, and chloro are tolerated by the reaction conditions employed. It is important to note that this method has a short reaction time (30 min in total) and represents an alternative approach for the synthesis of aryl sulfides over the existing protocols

Cross-Linked Fluorescent Supramolecular Nanoparticles for Intradermal Controlled Release of Antifungal DrugA Therapeutic Approach for Onychomycosis

The existing approaches to onychomycosis demonstrate limited success since the commonly used oral administration and topical cream only achieve temporary effective drug concentration at the fungal infection sites. An ideal therapeutic approach for onychomycosis should have (i) the ability to introduce antifungal drugs directly to the infected sites; (ii) finite intradermal sustainable release to maintain effective drug levels over prolonged time; (iii) a reporter system for monitoring maintenance of drug level; and (iv) minimum level of inflammatory responses at or around the fungal infection sites. To meet these expectations, we introduced ketoconazole-encapsulated cross-linked fluorescent supramolecular nanoparticles (KTZ⊂c-FSMNPs) as an intradermal controlled release solution for treating onychomycosis. A two-step synthetic approach was adopted to prepare a variety of KTZ⊂c-FSMNPs. Initial characterization revealed that 4800 nm KTZ⊂c-FSMNPs exhibited high KTZ encapsulation efficiency/capacity, optimal fluorescent property, and sustained KTZ release profile. Subsequently, 4800 nm KTZ⊂c-FSMNPs were chosen for <i>in vivo</i> studies using a mouse model, wherein the KTZ⊂c-FSMNPs were deposited intradermally <i>via</i> tattoo. The results obtained from (i) <i>in vivo</i> fluorescence imaging, (ii) high-performance liquid chromatography quantification of residual KTZ, (iii) matrix-assisted laser desorption/ionization mass spectrometry imaging mapping of KTZ distribution in intradermal regions around the tattoo site, and (iv) histology for assessment of local inflammatory responses and biocompatibility, suggest that 4800 nm KTZ⊂c-FSMNPs can serve as an effective treatment for onychomycosis