Tingting Li

The cross-dehydrogenative coupling of cyclic aldimines (C–H) and corresponding nucleophiles (X–H) provides one of the most straightforward synthetic methods for cyclic imidic acid derivatives. However, the method is currently limited to the cross-coupling of aldimines with amines to prepare amides. A robust and general synthetic method that enables the involvement of amines, alcohols, and even thiols as nucleophiles to divergently synthesize imidic acid derivatives is unknown. Herein, we disclose a carbene-catalyzed cross-dehydrogenative coupling between cyclic aldimines and amines, alcohols, and thiols, enabling efficient and divergent synthesis of cyclic imidic-acid-derived amidines, imidates, and imidothioates. The mild reaction conditions enable an excellent tolerance of various functional groups, allowing for the modification of complex natural products and pharmaceuticals. The practical utility of the current method is demonstrated by its successful application to the divergent synthesis of a wide range of substituted probenazole and dichlobentiazox (two marketed pesticide molecules).

An NHC-catalyzed dehaloacylation of α-bromo phosphonates for efficient access to α-substituted β-keto phosphonates was disclosed.

Planar chiral ferrocene-saccharide conjugates integrate multiple stereogenic elements and exhibit distinctive physicochemical and biological properties, rendering them highly attractive as chiral auxiliaries and diagnostic probes. However, their structural complexity─especially the intricate chirality and the requisite ester linkage─poses considerable synthetic challenges. Herein, we report an efficient N-heterocyclic carbene (NHC)-catalyzed strategy for the regioselective installation of prochiral ferrocene dicarboxaldehydes onto specific hydroxyl (OH) groups of unprotected saccharides. The synergistic combination of specific chiral NHC catalysts and boronic acids allows for simultaneous regioselectivity amplification and desymmetrization, affording ferrocene-saccharide conjugates with high regiocontrol and excellent planar chirality. This protocol operates under mild conditions and accommodates a broad range of ferrocene and saccharide substrates, thereby significantly expanding the accessible chemical space of planar-chiral ferrocene hybrids.

NHC and palladium cooperatively catalyzed efficient access to bioactive 5-acylated benzoxasilepines was disclosed.

BACKGROUND: Tobacco mosaic virus (TMV) is one of the most destructive plant pathogens. The modification of nucleosides is an effective method to develop anti‐TMV agents. A series of novel cytidine derivatives were designed and synthesized, and their antiviral activities against TMV were evaluated systematically. RESULTS: Activity assays revealed that 5z exhibited excellent protective and curative effects, with a half‐effective concentration (EC ₅₀ ) of 191.84 μg mL ⁻¹ , outperforming the control commercial agents ningnanmycin (240.79 μg mL ⁻¹ ) and ribavirin (622.22 μg mL ⁻¹ ). The mode of action (MoA) of 5z was thoroughly investigated through a multifaceted approach involving TMV‐GFP agrobacterium infiltration inoculation, chlorophyll content measurement, defense enzyme activity analysis and molecular docking. Mechanistic studies revealed that 5z exerts its multi‐target antiviral effects by specifically binding to the TMV coat protein (TMV‐CP), while simultaneously triggering the plant's defense enzyme system and boosting photosynthetic efficiency. CONCLUSION: Structure–activity relationships (SARs) were established for the cytidine derivatives, providing guidance for the design of cytidine‐based antiviral agents. Given its potent antiviral activity and unique mechanism of action, 5z shows strong promise as a novel antiviral agent. © 2026 Society of Chemical Industry.

An isothiourea-catalyzed acylative dynamic kinetic resolution reaction has been developed for the synthesis of chiral phthalidyl ester prodrugs.