PhI(OAc)-mediated aminoacyloxylation of β,γ-unsaturated hydrazones using Togni reagent II as an acyloxyl precursor.

A metal-free protocol for the direct construction of C(sp)-N and C-O bonds a PhI(OAc)-mediated dehydrogenative aminoacyloxylation of β,γ-unsaturated hydrazones with Togni reagent II is reported. Initiated by the carboxyl-containing species generated from Togni reagent II, this method offers a new solution for regioselective functionalization at a remote site on β,γ-unsaturated hydrazones, thus providing a straightforward method for the synthesis of acyloxyl-substituted pyridazines. This reaction features a broad substrate scope and mild conditions.

Annulative Aminosulfonylation of Unactivated Alkenes for Accessing Pyrazolines via Multicomponent SO Insertion.

A direct arylsulfonylation of β,γ-unsaturated hydrazones method, in which sulfonated pyrazolines are accessed by a three-component reaction of β,γ-unsaturated hydrazones, DABSO, and aryldiazonium tetrafluoroborates, has been developed without external oxidants or catalysts. This transformation is triggered by the formation of arylsulfonyl radicals in situ from the reaction of aryldiazonium tetrafluoroborates and DABSO, and is enabled by controllable generation of C center radical, in which DABSO was utilized as the sulfone source and an oxidant in this radical-mediated cascaded reaction. A wide range of substrates can be applied in this process to afford pyrazolines in good yield, and it is amenable for gram-scale synthesis.

Cyclin-dependent kinase 5 negatively regulates antiviral immune response by disrupting myeloid differentiation primary response protein 88 self-association.

As a member of the pattern recognition receptors (PRRs) involving in the innate immune system, Toll-like receptors (TLRs) can sense a wide range of microbial pathogens and combat infections by producing antimicrobial products, inflammatory cytokines, and chemokines. All TLRs, with the exception of TLR3, activate a signalling cascade via the myeloid differentiation primary response gene 88 (MyD88). Therefore, the activation of MyD88-dependent signalling pathway must be finely controlled.

Synthesis of α-allenic aldehydes/ketones from homopropargylic alcohols using a visible-light irradiation system.

A visible-light irradiation tandem oxidative aryl migration/carbonyl formation reaction, mediated by KSO and visible-light photoredox catalysis, has been discovered. The presented transformation provides a straightforward access to important α-allenic aldehyde/ketone derivatives from readily available homopropargylic alcohol derivatives in a regioselective manner of 1,4-aryl shift concomitant with carbonyl formation. The operational simplicity and broad substrate scope demonstrate the great potential of this method for the synthesis of highly functional α-allenic aldehyde/ketone derivatives.

Catalytic Oxidative Carbene Coupling of α-Diazo Carbonyls for the Synthesis of β-Amino Ketones via C(sp(3))-H Functionalization.

A catalytic domino oxidative carbene coupling (OCC) of α-diazo carbonyls has been established by treatment with N,N-dimethylanilines and carboxylic acids (or N-methylaniline) via direct C(sp(3))-H functionalization under convenient conditions. The reaction pathway is proposed to proceed through the sequence of carbene formation, enolization, and nucleophilic addition. The reaction enables de-diazotized carbo-oxygenation and carbo-amination of α-diazo carbonyls and provides practical access to α-(acyloxy)-β-amino ketones and α,β-diamino ketones.

[Analysis of characteristics of acute poisoning caused by various poisons in Guangxi, China].

Objective: To investigate the characteristics of acute poisonings caused by various poisons in Guangxi, China.

Methods: A retrospective investigation was performed in 5859 cases of acute poisonings who were admitted to 63 hospitals in 11 cities, as well as 531 types of poisons involved. The poisons were categorized into 6 groups; each group of cases was stratified by the rural or urban settings, frequency of poisoning, and cause of poisoning to analyze the numbers of cases and constituent ratios.

[Analysis of the characteristics of toxins in 6005 cases of acute poisoning in Guangxi].

Objective: To investigate the toxin characteristics of toxins in patients of acute poisoning in the Guangxi area.

Methods: A retrospective study was conducted. The data of acute poisoning cases and the causative toxins collected from 63 hospitals of Guangxi, including 36 city hospitals, 12 county hospitals, and 15 township health centers from January 2005 to December 2009 were collected.

[The comparative analysis of acute poisoning characteristics between cities and rural areas in Guangxi].

Objective: To compare the acute-poisoning characteristics between city and rural areas of Guangxi Province in order to provide clinical data for the formation of treatment strategies of acute poisoning in Guangxi.

Methods: Data of acute poisoning patients as treated in 36 municipal and 12 county hospitals, and also 15 rural clinics in 11 cities of Guangxi during 2005 to 2009 were collected and analyzed according to poisoning population, poisoning site, poisoning process, and poisoning degree.

Results: By analysing 3678 and 2153 cases of acute poisoning patients in rural and urban areas, the gender [χ (2) = 5.

LTB4 can directly stimulate human osteoclast formation from PBMC independent of RANKL.

Leukotriene B4, as a kind of 5-lipoxygenase metabolite of arachidonic acid, is known to influence osteoclast formation and bone resorption. In order to determine whether Leukotriene B4 could directly stimulate human osteoclast differentiation and activation independent of RANKL (ODF), three different concentrations of Leukotriene B4 (10(-9)M, 10(-8)M, 10(-7)M) were added to the culture of CD14+ monocyte fraction of peripheral blood mononuclear cell (PBMC) in the presence of macrophage colony-stimulating factor (M-CSF). Under these conditions, Leukotriene B4 could induce multinucleated cells, which were positive for Tartrate-resistant acidic phosphatase (TRAP) staining and capable of bone resorption.

[Significance and role of increased expression of extracellular matrix metalloproteinase induced in the aseptic loosening of prostheses].

Objective: To investigate the expression of extracellular matrix metalloproteinase induced (EMMPRIN) in the interface tissue, and explore the role of EMMPRIN in the aseptic loosening of prostheses.

Methods: Immunohistochemistry was performed to characterize the EMMPRIN-expressing cells at sites of interface tissue around aseptic loosened hip prostheses in 16 cases. Reverse transcription-polymerase chain reaction (RT-PCR) was performed to study the existence of EMMPRIN mRNA in interface tissue samples.