This paper delves into the intricate relationship between changes in Magnetic inclination and declination at specific geographical locations and the navigational decisions of migratory birds. Leveraging a dataset sourced from a prominent bird path tracking web resource, encompassing six distinct bird species' migratory trajectories, latitudes, longitudes, and observation timestamps, we meticulously analyzed the interplay between these avian movements and corresponding alterations in Magnetic inclination and declination. Employing a circular von Mises distribution assumption for the latitude and longitude distributions within each subdivision, we introduced a pioneering circular-circular regression model, accounting for von Mises error, to scrutinize our hypothesis.
View Article and Find Full Text PDFThe straightforward and rapid incorporation of a thiazolidinedione scaffold into prefunctionalized (hetero)aromatic compounds is in demand for the development of antidiabetic glitazones and other pharmaceuticals. Herein, we report the unprecedented N- and O-directed C-H alkylation of various (hetero)arenes with methylene thiazolidinediones under rhodium(III) catalysis. The applicability of the developed protocol in challenging contexts is exhibited by the late-stage installation of a methylene thiazolidinedione moiety on the C-H bond of commercially available drug molecules.
View Article and Find Full Text PDFThe ruthenium(II)-catalyzed tandem C-H allylation and intramolecular dipolar cycloaddition between azomethine imines and 2-methylidenetrimethylene carbonate is described herein. The initially formed β-substituted allyl fragment could trigger the exotype [3 + 2] cycloaddition with the polar azomethine group, resulting in the formation of bridged tetracycles bearing a hydroxymethylene group at a bridgehead carbon center. A wide substrate scope and broad functional group compatibility were observed.
View Article and Find Full Text PDFThe C3-selective homodimerization of quinoxalinones is described. A C3-sp carbanion species generated through deprotonation of quinoxalinone using potassium -butoxide (KOBu) transfers an electron (single electron transfer mechanism) to a second quinoxalinone, affording a radical-anion intermediate. The radical scavenging and electron paramagnetic resonance (EPR) experiments support the plausible radical reaction pathway.
View Article and Find Full Text PDFThe site-selective and metal-free C-H nitration reaction of quinoxalinones and pyrazinones as biologically important N-heterocycles with t-butyl nitrite is described. A wide range of quinoxalinones were efficiently applied in this transformation, providing C7-nitrated quinoxalinones without undergoing C3-nitration. From the view of mechanistic point, the radical addition reaction exclusively occurred at the electron-rich aromatic region beyond electron-deficient N-heterocycle ring.
View Article and Find Full Text PDFThe rhodium(III)-catalyzed spiroannulation reaction between -aryl indazol-3-ols and maleimides is described herein. The developed method is showcased by the construction of spirosuccinimides using bioactive molecule-linked and chemical probe-linked maleimides. Combined mechanistic investigations including the determination of an isolable rhodacycle complex aided the elucidation of a plausible reaction mechanism.
View Article and Find Full Text PDFThe Rh(III)-catalyzed C-H functionalization and subsequent oxidative annulation between 5-aryl pyrazinones and internal alkynes are reported. This protocol provides facile access to a wide range of pyrazinone-linked naphthalenes via the C(sp)-H alkenylation and subsequent annulation. This transformation is characterized by mild conditions, simplicity, and excellent functional group compatibility.
View Article and Find Full Text PDFThe direct functionalization of -heterocycles is a vital transformation for the development of pharmaceuticals, functional materials, and other chemical entities. Herein, the transition-metal-free alkylation and acylation of C(sp)-H bonds in biologically relevant 2-benzoxazinones with 1,4-dihydropyridines as readily accessible radical surrogates is described. Excellent functional group compatibility and a broad substrate scope were attained.
View Article and Find Full Text PDFObjectives: This systematic review aims to provide insight into the outcome of extracorporeal membrane oxygenation (ECMO) and invasive mechanical ventilation use in critically ill COVID-19 patients.
Data Sources: Electronic databases PubMed Central and PubMed were searched from January 2020 to June 2020 for published studies about ECMO and/or invasive mechanical ventilation use in COVID-19 patients. Data Extraction and Study Selection: The search strategy retrieved 766 articles, of which 19 studies consisting of 204 patients fulfilled the inclusion criteria and were included in the analysis.
The Rh(III)-catalyzed C-H functionalization and subsequent intramolecular cyclization between azobenzenes and vinylene carbonate is described herein. Depending on the electronic property of azobenzenes, this transformation results in the formation of (2)-indazoles or dihydrocinnolin-4-ones through the generation of -alkylated azo-intermediates followed by decarboxylation. Surprisingly, vinylene carbonate acts as an acetaldehyde or acetyl surrogate to enable the [4 + 1] or [4 + 2] annulation reaction.
View Article and Find Full Text PDFFibroblast activation protein (FAP) belongs to the family of prolyl-specific serine proteases and displays both exopeptidase and endopeptidase activities. FAP expression is undetectable in most normal adult tissues, but is greatly upregulated in sites of tissue remodeling, which include fibrosis, inflammation and cancer. Due to its restricted expression pattern and dual enzymatic activities, FAP inhibition is investigated as a therapeutic option for several diseases.
View Article and Find Full Text PDFA redox-neutral C2-selective methylation of heterocyclic -oxides with sulfonium ylides is described herein. This report presents unprecedented findings for the utility of sulfonium ylides as the methylation source of -heterocycles beyond the Corey-Chaykovsky reaction. Intriguingly, pyrrolidine plays a significant role in minimizing the reductive C2-methylation process.
View Article and Find Full Text PDFThe direct methylation of N-heterocycles is an important transformation for the advancement of pharmaceuticals, agrochemicals, functional materials, and other chemical entities. Herein, the unprecedented C(sp )-H methylation of iminoamido heterocycles as nucleoside base analogues is described. Notably, trimethylsulfoxonium salt was employed as a methylating agent under aqueous conditions.
View Article and Find Full Text PDFIn this study, we aim to assess the association of dengue viremia with dengue severity. The study protocol was developed and registered in PROSPERO (CRD42016039864). We searched nine databases to find potential papers.
View Article and Find Full Text PDFThe preparation of phthalazinone derivatives is pivotal for their utilization as pharmaceutical agents and other entities. Herein, we report the phthalazinone-assisted carbon-nitrogen bond forming reaction using dioxazolones as robust amidation sources under Rh(III) catalysis. The broad functional group tolerance and complete site-selectivity are observed.
View Article and Find Full Text PDFA transition-metal-free deoxygenative C-H amination reaction of azine--oxides with acyl azides is described. The initial formation of an isocyanate from the starting acyl azide via a Curtius rearrangement can trigger a [3 + 2] dipolar cycloaddition of polar -oxide fragments to generate the aminated azine derivative. The applicability of this method is highlighted by the late-stage and sequential amination reactions of complex bioactive compounds, including quinidine and fasudil.
View Article and Find Full Text PDFRuthenium(II)-catalyzed C(sp)-H functionalization of -aryl phthalazinones with a range of aldehydes and activated ketone is described. Initial formation of hydroxyalkylated phthalazinones and subsequent Mitsunobu cyclization provided facile access to biologically relevant indazolophthalazinones. The utility of this method is highlighted by synthetic transformations into a series of potentially bioactive scaffolds.
View Article and Find Full Text PDFThe synthesis of alkylated diazine derivatives is important for their practical utilization as pharmaceuticals and for other purposes. Herein, we describe the metal-free site-selective C-H alkylation of diazine -oxides using phosphonium ylides that affords a variety of alkylated diazine derivatives with broad functional group tolerance. The utility of this method is showcased by the late-stage functionalization of a commercially available drug such as varenicline.
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