The modular synthesis of structurally unique dragocins A—C (1—3) and their analogues, characterized by an uncommon tri-oxa-tricyclic[6.2.1]undecane skeleton and the presence of a heteroatomic substituent at the C-4' position, has been successfully achieved using commercially available and inexpensive anisomycin and D-ribofuranosyl thioglycoside derivative as the starting materials. The construction of the tri-oxa-tricyclic[6.2.1]undecane moiety involved the stereoselective formation of the β-ribofuranosidic bond and DDQ-promoted intramolecular cross-dehydrogenative etherification. Additionally, the equipment of a chlorine atom and a methoxy group at the tertiary C-4' position was accomplished through a silver-catalyzed radical decarboxylative chlorination reaction and an electrophilic etherification reaction of the enol intermediate. The cytotoxicity assessment indicated that demethyl dragocin A (28), the N-demethylated derivative of dragocin A, may serve as a promising anticancer candidate. More details are discussed in the article by Li et al. on pages 1107—1113.

An electrochemical method is developed for the direct decarboxylative phosphorylation of α-amino acids to α-amino phosphonates using continuous-flow electrochemistry. The method eliminates the need for strong oxidants and multi-step processes, offering a straightforward and scalable approach. Key to its success is the establishment of a microenvironment on the anode surface in acidic conditions, facilitating selective decarboxylation and C—P bond formation. More details are discussed in the article by Xu et al. on pages 1167—1172.

Based on synthesis and cytotoxicity evaluation of dragocins A—C and their congeners, a potential anticancer agent has been identified.

A series of shelf-stable monofluoroalkylated sulfonium ylide reagents was developed, providing a robust approach for the preparation of monofluoroalkylated ethers, sulfonates, and esters with a variety of O-nucleophiles including phenols, sulfonic acids, carboxylic acids,1-hydroxy-benzotrizoles and amino acids in good to excellent yields. Further expansion of monofluoroalkylation of C-terminus of peptides potentially provided modified drug-like peptides.

This work reports an unappreciated C(sp²)−C(sp³) construction on the polyaromatic rings involving [Ni]/[Co] bimetallic C−H alkylation strategy. In this protocol, a cobalt-catalyzed homolysis of alkyl chlorides is responsible for the radical generation, while a Ni(II)→Ni(III)→Ni(I) cycle enables the C8−H insertion of alkyl radicals to the polyaromatics. Good functional group tolerance and potential product diversification promote the late stage functionalization on complex bioactive molecules.

This research introduces a visible-light photocatalytic strategy for the dearomatization of indole derivatives containing amide groups, yielding spiroindolines with high diastereoselectivity (> 20 : 1). The process is driven by energy transfer, enabling the activation of amide functionalities through triplet excited-state intramolecular proton transfer (T-ESPT). Density Functional Theory (DFT) calculations reveal key π-π stacking interactions between the indole core and pyridine ring, as well as enhanced hydrogen bonding between pyridine nitrogen and hexafluoroisopropanol (HFIP) in the triplet excited state, facilitating this transformation. The method offers a new avenue for dearomative reactions involving amide groups.

We developed a novel Pd-catalyzed carbonylation of ortho-alkenyl iodobenzenes with CO, affording a diverse array of 3-arylindenones in good to excellent yields (up to 94% yield). This methodology exhibits broad substrate scope and good functional group compatibility. The synthetic utility was demonstrated by a gram-scale reaction, diverse product derivatizations, and the preparation of an intermediate for a PPARγ agonist.

The self-assembly phenomenon of KAUST-7 crystals was observed under different synthetic routes. The adsorption capacity of C₃H₆ on KAUST-7-MS was 53% higher than that of KAUST-7. It concurrently combines an excellent C₃H₆/C₃H₈ uptake ratio of 3.1 and kinetic selectivity (96.5) for C₃H₆/C₃H₈ separation with an equilibrium-kinetic combined selectivity of 42.5.

The strategic incorporation of eC9-2Cl as a weak absorptive third component into the D18-Cl:F-BTA3 system of indoor organic photovoltaic (OPV) cells markedly influences energy transfer and exciton dissociation, pivotal processes for OPV performance. This advancement addresses the challenges of indoor light harvesting and sets a new benchmark for high-performance indoor OPV design.

A novel and efficient method for selective synthesis of bromo-substituted 2H-pyrroles and 3H-pyrroles has been achieved from 1,3-enynes, NBS and TMSN₃ via H₂O-promoted cyclization reactions or TFA-catalyzed cyclization/2,3-shift reactions, providing a range of structurally diverse products in moderate to good yields under mild conditions.

We have developed a tandem approach that assembles simple β-chloroethylphosphane, alkynyl imines (or alkynyl ketones), and nitrones into structurally complex isoxazolidine fused phospholene scaffolds through a sequential process involving phospha-Michael addition, intramolecular cyclization and dearomative [3+2] cycloaddition reactions.

Reported herein is an electrochemical method for the direct decarboxylative phosphorylation of α-amino acids to α-amino phosphonates. This method bypasses the need for strong chemical oxidants and 2-step processes involving preliminary conversions, making it a more straightforward synthetic tool.

Two tetraphenylethene-based tetraimidazolium cyclophanes 1 and 2 were synthesized via a one-step S_N2 reaction. These cyclophanes can form 1 : 1 host-guest complexes with nucleoside triphosphates in water and exhibit selective recognition for GTP with distinct fluorescence responses.

The ligand-controlled [3+2]/[4+2] cycloadditions between zwitterionic π-propargyl palladium species originated from vinylidenecyclopropane-diesters with benzofulvenes were demonstrated for a divergent synthesis of spiroindenes. Moderate to excellent yields along with good functional group compatibility and a broad substrate scope were achieved.

The polar [NH₄]M(HCO₂)₃ frameworks exhibit dielectric relaxation due to orientational disorder of the NH₄, as identified by a multi-technique examination of their structure and dynamics.

The optoelectronic properties of COFs can be predicted by theoretical calculation. With the computational prediction, the thiophene-based D-A COFs with the best photocatalytic hydrogen production can be readily prepared and experimentally validated. We have demonstrated here a time- and cost-saving approach for rational design of COFs with desired properties.

A regioselective C8−H alkylation strategy with inert alkyl chloride on polyaromatics has been reported. Inexpensive transition metals nickel and cobalt enable access to various C8-substituted polyaromatic products with good yields, suggesting a potential late-stage functionalization of naphthalene-based natural products and bioactive molecules. In the two-phase mechanism, cobalt is responsible for radical generation, and nickel undergoes the C8−H insertion. More details are discussed in the article by Zhang and Mao et al. on pages 1121—1128.

This study presents an approach for the visible-light photocatalytic intramolecular dearomatization of indole derivatives containing amide groups. By harnessing energy transfer, the method enables the formation of hydroxyl-substituted spiroindolines under mild conditions, achieving high diastereoselectivity and moderate to high yields. Mechanistic investigations reveal that the reaction proceeds through a triplet excited state intermolecular proton transfer (T-ESPT) enabled by energy transfer. More details are discussed in the article by Fu et al. on pages 1129—1134.