Synthesis of Polyfluoroalkyl Aryl Ethers Mediated by Sulfuryl Fluoride as a Traceless Activator.

Herein, we report the metal-free synthesis of polyfluoroalkyl aryl ethers via nucleophilic substitution of fluorosulfonates, obtained in one pot by bubbling of sulfuryl fluoride (SOF). Polyfluoroalkyl aryl ethers are present in a variety of biologically active compounds, but previous methods for accessing them required metal catalysts or harsh conditions. With this method, their synthesis is possible under mild conditions and with a short reaction time (30 min) from commercially available starting materials and in yields of ≤97%.

Phenylseleno trifluoromethoxylation of alkenes.

Trifluoromethoxylated molecules and selenylated compounds find a wide range of interesting applications, but separately. In order to combine the potential of these two motifs and to propose a new class of compounds, we have developed an electrophilic phenylseleno trifluoromethoxylation of alkenes, which leads to β-selenylated trifluoromethoxylated compounds or, upon subsequent reduction, to the trifluoromethoxylated ones.

A platform for rapid patient-derived cutaneous neurofibroma organoid establishment and screening.

Localized cutaneous neurofibromas (cNFs) are benign tumors that arise in the dermis of patients affected by neurofibromatosis type 1 syndrome. cNFs are benign lesions: they do not undergo malignant transformation or metastasize. Nevertheless, they can cover a significant proportion of the body, with some individuals developing hundreds to thousands of lesions.

State-of-the-Art Review on Botanical Hybrid Preparations in Phytomedicine and Phytotherapy Research: Background and Perspectives.

Background: Despite some evidence supporting the synergy concept, the commonly known assumption that combinations of several herbs in one formulation can have better efficacy due to additive or synergistic effects has yet to be unambiguously and explicitly studied.

Study Aim: The study aimed to reveal the molecular interactions in situ of host cells in response to botanical hybrid preparations (BHP) intervention and justify the benefits of implementing BHP in clinical practice.

Results: This prospective literature review provides the results of recent clinical and network pharmacology studies of BHP of L.

Efficacy of Kan Jang in Patients with Mild COVID-19: A Randomized, Quadruple-Blind, Placebo-Controlled Trial.

. This study aimed to assess the efficacy of the treatment of Kan Jang, a fixed combination of (Burm. F.

New Chemical Transformations Involving SO F -Mediated Alcohol Activation.

Sulfuryl fluoride is a gas produced on a multi-ton scale for its use as a fumigant. In the last decades, it has gained interest in organic synthesis as a reagent with unique properties in terms of stability and reactivity when compared to other sulfur-based reagents. Sulfuryl fluoride has not only been used for sulfur-fluoride exchange (SuFEx) chemistry but also encountered applications in classic organic synthesis as an efficient activator of both alcohols and phenols, forming a triflate surrogate, namely a fluorosulfonate.

Development of a Standardised System to Classify Injury-Inciting Circumstances in Football: the Football Injury Inciting Circumstances Classification System (FIICCS).

Background: A comprehensive examination of the sport-specific activities and circumstances being performed at the time of injury is important to hypothesise mechanisms, develop prevention strategies and inform future investigations. Results reported in the literature are inconsistent because inciting activities are reported using different classifications. Hence the aim was to develop a standardised system for the reporting of inciting circumstances.

Ruthenium-Catalyzed Synthesis of Aryl and Alkenyl Halides from Fluorosulfonates.

Aryl and alkenyl halides are widely used as key intermediates in organic synthesis, particularly for the formation of organometallic reagents or as radical precursors. They are also found in pharmaceutical and agrochemical ingredients. In this work, the synthesis of aryl and alkenyl halides from the corresponding fluorosulfonates using commercially available ruthenium catalysts is reported.

Exploring F/CF substituted oxocarbenium ions for the diastereoselective assembly of highly substituted tetrahydrofurans.

Understanding the influence of emerging fluorinated motifs is of a crucial importance in the context of the exponentially growing exploitation of fluorine in many fields. Herein, we report on the dramatic effect of a local partial charge inversion by replacing a CHCH group by a CFCF. This strategy allows the diastereoselective reduction of 5-membered ring oxocarbenium ions to access highly substituted tetrahydrofurans.

Traceless N-Polyfluoroalkylation of Weakly Nucleophilic Nitrogen Containing Compounds.

Here we report an efficient access to high-value N-polyfluoroalkyl anilines, primary polyfluoroalkylamines and N,N-bis(polyfluoroalkyl)amines, via N-polyfluoroalkylation of sulfonamides and phthalimide derivatives using sulfuryl fluoride (SO F ). The in situ formation of polyfluoroalkyl fluorosulfonates from commercially available fluorinated alcohols and economical sulfuryl fluoride is highly advantageous given that some polyfluoroalkyl halides are ozone-depleting substances (ODS) regulated by the Montreal protocol. This general method is applied to the polyfluoroalkylation of a variety of sulfonamides, N-sulfonyl carbamates and phthalimide with a wide tolerance of functional groups.

Direct Deprotonative Functionalization of α,α-Difluoromethyl Ketones using a Catalytic Organosuperbase.

The deprotonative functionalization of α,α-difluoromethyl ketones is described herein. Using a catalytic organosuperbase and a silane additive, the corresponding difluoroenolate could be generated and trapped with aldehydes to deliver various α,α-difluoro-β-hydroxy ketones in high yields. This new strategy tolerates numerous functional groups and represents the access to the difluoroenolate by direct deprotonation of the difluoromethyl unit.

Network Pharmacology of Ginseng (Part III): Antitumor Potential of a Fixed Combination of Red Ginseng and Red Sage as Determined by Transcriptomics.

Background: This study aimed to assess the effect of a fixed combination of Red Ginseng and Red Sage (RG-RS) on the gene expression of neuronal cells to evaluate the potential impacts on cellular functions and predict its relevance in the treatment of stress and aging-related diseases and disorders.

Methods: Gene expression profiling was conducted by transcriptome-wide mRNA microarray analyses of murine HT22 hippocampal cell culture after treatment with RG-RS preparation. Ingenuity pathway analysis (IPA) was performed with datasets of significantly upregulated or downregulated genes and the expected effects on the physiological and cellular function and the diseases were identified.

Ketenimines as Intermediates To Access Difluoromethoxylated Scaffolds.

We report herein the generation of difluoromethoxylated ketenimines. This novel intermediate is readily obtained from the corresponding oxime through a Beckmann rearrangement. The reactivity potential of this species is demonstrated as it easily undergoes addition of various nucleophiles, with a great modularity of the starting oxime.

Network Pharmacology of Adaptogens in the Assessment of Their Pleiotropic Therapeutic Activity.

The reductionist concept, based on the ligand-receptor interaction, is not a suitable model for adaptogens, and herbal preparations affect multiple physiological functions, revealing polyvalent pharmacological activities, and are traditionally used in many conditions. This review, for the first time, provides a rationale for the pleiotropic therapeutic efficacy of adaptogens based on evidence from recent gene expression studies in target cells and where the network pharmacology and systems biology approaches were applied. The specific molecular targets and adaptive stress response signaling mechanisms involved in nonspecific modes of action of adaptogens are identified.

One-step Oxidative Monofluorination of Electron-Deficient Sulfoxides to Access Highly Lewis Acidic Sulfur(VI) Cations.

The strongly oxidizing, powerful electrophilic fluorination reagent [FXe][OTf] is shown to effect direct oxidative monofluorination of sulfoxides. This one-step, chloride promoter-free methodology provides access to so far inaccessible, yet highly desirable strongly Lewis acidic fluorosulfoxonium cations from electron-deficient and/or sterically demanding sulfoxides that are shown to be practically unreactive towards the previously reported XeF /NEt Cl system. Experimental and density functional theory studies have been conducted to assess the Lewis acidities of the prepared sulfur(VI) cations.

Efficacy of Kan Jang in Patients with Mild COVID-19: Interim Analysis of a Randomized, Quadruple-Blind, Placebo-Controlled Trial.

Kan Jang, the fixed combination of (Burm. F.) Wall.

Cortical Anoxic Spreading Depolarization During Cardiac Arrest is Associated with Remote Effects on Peripheral Blood Pressure and Postresuscitation Neurological Outcome.

Background: Spreading depolarizations (SDs) are self-propagating waves of neuronal and glial depolarizations often seen in neurological conditions in both humans and animal models. Because SD is thought to worsen neurological injury, the role of SD in a variety of cerebral insults has garnered significant investigation. Anoxic SD is a type of SD that occurs because of anoxia or asphyxia.

Study of Carbamoyl Fluoride: Synthesis, Properties and Applications.

Carbamoyl fluoride is a fluorinated group that, to this date, remains underexplored, probably due to the lack of data concerning its properties. In this paper, a study of carbamoyl fluoride is presented. Stability studies, in particular under physiological conditions, and lipophilicity measurement were performed.

Formation of synthetically relevant CF-substituted phenonium ions in superacid media.

Predestined to be transient theoretical species, phenonium ions can now be considered as cationic intermediates of choice in organic synthesis. Here, we demonstrate that under non-nucleophilic and superacidic conditions, CF-substituted phenonium ions can be generated to furnish original CF-substituted dihydrostilbenes of interest.

Efficacy of Adaptogens in Patients with Long COVID-19: A Randomized, Quadruple-Blind, Placebo-Controlled Trial.

Currently, no effective treatment of comorbid complications or COVID-19 long-haulers during convalescence is known. This randomized, quadruple-blind, placebo-controlled trial aimed to assess the efficacy of adaptogens on the recovery of patients with Long COVID symptoms. One hundred patients with confirmed positive SARS-CoV-2 test, discharged from COVID Hotel isolation, Intensive Care Unit (ICU), or Online Clinics, and who experienced at least three of nine Long COVID symptoms (fatigue, headache, respiratory insufficiency, cognitive performance, mood disorders, loss of smell, taste, and hair, sweatiness, cough, pain in joints, muscles, and chest) in the 30 days before randomization were included in the study of the efficacy of Chisan/ADAPT-232 (a fixed combination of adaptogens Rhodiola, Eleutherococcus, and Schisandra) supplementation for two weeks.

Early intervention with Kan Jang® to treat upper-respiratory tract infections: A randomized, quadruple-blind study.

Background And Aim: and preparations and their fixed combination, called Kan Jang®, are traditionally used for relieving symptoms of upper-respiratory tract infections (URTIs). This study aimed to assess the efficacy of early intervention with Kan Jang® on the relief and duration of inflammatory symptoms during the acute phase of the disease.

Experimental Procedure: A total of 179 patients with URTI symptoms received six Kan Jang® (daily dose of andrographolides: 60 mg) or placebo capsules a day for five consecutive days in this randomized, quadruple-blinded, placebo-controlled, two-parallel-group phase II study.

Network Pharmacology of Ginseng (Part II): The Differential Effects of Red Ginseng and Ginsenoside Rg5 in Cancer and Heart Diseases as Determined by Transcriptomics.

C.A.Mey.