ConspectusActivation of inert chemical bonds, such as C–H, C–O, C–C, and so on, is a very important area, to which has been drawn much attention by chemists for long time viewed one the most ideal ways produce valuable chemicals. Under modern bond activation logic, many conventionally "inert" bonds that were intact under traditional conditions can be reconsidered novel functionalities, not only avoids tedious synthetic procedures prefunctionalizations emission undesirable wastes but also...

Speeding up borylation Catalytic is the rare reaction that can selectively target stronger over weaker saturated carbon–hydrogen (C–H) bonds. However, trade-off has been slow and requires high excess of hydrocarbon. Oeschger et al. now report right ligand (2-methylphenanthroline) coordinated to iridium accelerate by 50- 80-fold. This rate enhancement enables selective primary C–H bonds with hydrocarbon as limiting reagent. The also unusually for β-C–H in heterocycles. Science , this issue p. 736

Disinfection of hazardous microorganisms that may challenge environmental safety is a crucial issue for economic and public health. Here, we explore the potential novel electrochemical disinfectant named plasma activated water (PAW), which was generated by nonthermal plasma, inactivating Staphylococcus aureus (S. aureus). Meanwhile, influence bovine serum albumin (BSA) on PAW disinfection efficacy investigated. In presence BSA, treatments achieved reduction S. ranging from 2.1 to 5.5 Log,...

We report the incorporation of large substituents based on heavy main-group elements that are atypical in ligand architectures to enhance dispersion interactions and, thereby, enantioselectivity. Specifically, we prepared chiral biaryl bisphosphine (TMG-SYNPHOS) containing 3,5-bis(trimethylgermanyl)phenyl groups phosphorus and applied this challenging problem enantioselective hydrofunctionalization reactions 1,1-disubtituted alkenes. Indeed, TMG-SYNPHOS forms a copper complex catalyzes...

Abstract The borylation of C−H bonds catalyzed by transition metals has been investigated extensively in the past two decades, but no iridium‐catalyzed enantioselective reported. We report a set borylations aromatic bonds. This reaction relies on newly developed chiral quinolyl oxazoline ligands. process proceeds under mild conditions with good to excellent enantioselectivity, and borylated products can be converted enantioenriched derivatives containing new C−O, C−C, C−Cl, or C−Br

We report highly enantioselective intramolecular, silylations of unactivated, primary C(sp3)–H bonds. The reactions form dihydrobenzosiloles in high yields with excellent enantioselectivities by functionalization enantiotopic methyl groups under mild conditions. reaction is catalyzed an iridium complex generated from [Ir(COD)OMe]2 and chiral dinitrogen ligands that we recently disclosed. C–Si bonds the enantioenriched were further transformed to C–Cl, C–Br, C–I, C–O final products. potential...

Abstract Transition‐metal‐catalyzed enantioselective P−C cross‐coupling of secondary phosphine oxides (SPOs) is an attractive method for synthesizing P ‐stereogenic phosphorus compounds, but the development such a dynamic kinetic asymmetric process remains considerable challenge. Here we report unprecedented highly intermolecular coupling SPOs and aryl iodides catalyzed by copper complexes ligated finely modified chiral 1,2‐diamine ligand. The reaction tolerates wide range iodides, affording...

Racemic phenanthroindolizidine alkaloids tylophorine, antofine, and deoxytylophorinine, optically pure S-(+)-tylophorine R-(−)-tylophorine were synthesized evaluated for their antiviral activities against tobacco mosaic virus (TMV). Further salinization modifications based on tylophorine increased stability water solubility improved the activity in application. The bioassay results showed that most of these compounds higher TMV vitro vivo than commercial Ningnanmycin. Especially, salt...

The functionalization of unactivated C(sp3)–H bonds aliphatic amines catalyzed by transition-metal complexes is important because amine-based functionality present in a majority biologically active molecules and commercial pharmaceuticals. However, such reactions are underdeveloped challenging to achieve general the basicity reducing properties alkylamines tends interfere with potential reagents catalysts. C–H β nitrogen form prevalent 1,2-amino functionalized structures particularly bond...

Iridium catalysts containing dative nitrogen ligands are highly active for the borylation and silylation of C-H bonds, but chiral analogs these enantioselective reactions have not been developed. We report a new pyridinyloxazoline ligand enantioselective, intramolecular symmetrical diarylmethoxy diethylsilanes. Regioselective unsymmetrical substrates was also achieved in presence this newly developed system. Preliminary mechanistic studies imply that bond cleavage is irreversible,...

// Bo Su 1, 2, 3, * , Jian 4, Ying Zeng Fang Liu 2 Hong Xia Yan-Hua Ma Zhi-Gang Zhou Shuo Zhang Bang-Min Yang You-Hua Wu 1 Xi Xiao-Hong Ai Hui Ling Hao Jiang Qi Center for Gastric Cancer Research of Hunan Province, First Affiliated Hospital, University South China, Hengyang, 421001 Hunan, China Key Laboratory Cellular and Molecular Pathology Provincial University, Institute, 3 Pharmacoproteomics Institute Pharmacy Pharmacology, 4 Department Pathology, Second These authors have contributed...

Site-selective functionalizations of C–H bonds are often achieved with a directing group that leads to five- or six-membered metallacyclic intermediates. Analogous reactions occur through four-membered metallacycles rare. We report challenging palladium-catalyzed oxidation primary β nitrogen in an imine aliphatic amine, process occurs palladacyclc intermediate. The success the reaction relies on identification, by H/D exchange, simple (salicylaldehyde) capable inducing formation this small...

The development of a single catalyst system that enables cascade reaction processes involving multiple components to occur in highly chemo-, regio-, and enantioselective manner presents significant challenge catalysis. Here, we introduce direct catalytic asymmetric synthesis enantioenriched secondary homoallyl borons by assembling four readily available components─terminal alkynes, boron reagents (HBdan), silyl hydrides (PMHS), allyl electrophiles─in hydroboration hydroallylation sequence....

Compounds bearing both boryl and amino groups at distal positions are invaluable synthons for synthesizing pharmaceuticals, drug candidates, natural products, but their catalytic enantioselective synthesis remains rarely explored. We report the first 1,4-borylamination reaction through a copper-catalyzed cascade hydroborylation hydroamination of arylidenecyclopropanes. This combines four readily available components in highly chemo-, site-, fashion (>20:1 r.r. up to 99% ee), yielding diverse...

Background The prevalence of metabolic dysfunction-associated steatotic liver disease (MASLD) continues to rise each year, posing a significant threat people in their physical and mental health, as well imposing considerable economic burden on healthcare systems. Furthermore, activity (PA) is recognized one the effective strategies for prevention MASLD. However, epidemiological evidence association between weekend warriors’ (WWs) exercise modes MASLD inconsistent. primary objective this...

An efficient and green intramolecular oxidative phenol coupling for the direct construction of spirocyclohexadienones has been developed, which uses environment-friendly sodium nitrite as catalyst oxygen in air terminal oxidant. Hydroxy-containing substituted phenanthrenes dibenzoazepines could be easily obtained from dienone–phenol rearrangement.

Our recent investigation on the antiviral activities against tobacco mosaic virus (TMV) of phenanthroindolizidine alkaloid analogues preliminarily revealed that basic skeleton and substitution pattern at C13a position molecule, which are closely related to spatial arrangement have great effects biological activity. To further study in-depth influence configuration three-dimensional (3D) conformation molecules their anti-TMV structure-activity relationship (SAR), a series D-ring opened...

Abstract In the context of transition‐metal‐catalyzed CH functionalization, directing‐group strategy was developed for improvement chemical reactivity and selectivity. Recently, to avoid inherent limitations traditional mono‐role directing groups, a dual‐role oxidizing‐directing‐group developed, in which group acts both as oxidant. Herein, we report multirole group, possesses multiple reactive sites, exhibits unique selectivity, leads four different types products from single starting...

peri-Disubstituted naphthalenes exhibit interesting physical properties and unique chemical reactivity, due to the parallel arrangement of bonds two peri-disposed substituents. Regioselective installation a functional group at position peri 1-substituted is challenging steric interaction between existing substituent which second one would be installed. We report an iridium-catalyzed borylation C-H bond silyl in analogous polyaromatic hydrocarbons. The reaction occurs under mild conditions...

Abstract The borylation of C−H bonds catalyzed by transition metals has been investigated extensively in the past two decades, but no iridium‐catalyzed enantioselective reported. We report a set borylations aromatic bonds. This reaction relies on newly developed chiral quinolyl oxazoline ligands. process proceeds under mild conditions with good to excellent enantioselectivity, and borylated products can be converted enantioenriched derivatives containing new C−O, C−C, C−Cl, or C−Br

Corrected by: A Simple and Efficient Oxidative Coupling of Aromatic Nuclei Mediated by Manganese DioxideSynthesis 2013; 45(18): 2626-2626DOI: 10.1055/s-0033-1338536