An expedient solvent-free synthesis of 2-deoxy-2-bromo-hexopyrano-β-nucleosides stereo- and regioselectively from protected glycals and unactivated nucleobases using cheaper and easily available reagent systems has been developed. The synthesis is mediated by a Lewis acid and is solvent-free. The substrate scope of the reaction was analysed with ether, ester and silyl-protected glycals as donors and different pyrimidine and purine bases were taken into consideration.
View Article and Find Full Text PDFTrifluoromethanesulfonic anhydride (TfO) exhibits excellent reactivity as an electrophile, serving as a highly versatile reagent in diverse chemical transformations. Herein, we report an operationally simple, efficient, unique, and practical one-step strategy for synthesizing diverse valuable structures bearing furo[3,2-]furans core leveraging TfO's promoted reactivity of nitriles with diacetonide protected furanose. Furthermore, we demonstrate the potential of furo[3,2-]furan as a precursor for complex structures through 1,3-dipolar cycloaddition.
View Article and Find Full Text PDFHerein, we present two unprecedented reactions for the synthesis of γ-butenolides and oxazoles, leveraging TfO's promoted reactivity of nitriles with diacetonide endoglucofuranose and 1,2,3,5-tetra--acetyl-β-d-ribofuranose. This method is highly efficient and straightforward and employs a one-step, metal-free protocol. It is effective with both aromatic and aliphatic nitriles and demonstrates a broad substrate scope.
View Article and Find Full Text PDFIn recent years, we and others have identified a number of enhancers that, when incorporated into rAAV vectors, can restrict the transgene expression to particular neuronal populations. Yet, viral tools to access and manipulate fine neuronal subtypes are still limited. Here, we performed systematic analysis of single cell genomic data to identify enhancer candidates for each of the cortical interneuron subtypes.
View Article and Find Full Text PDFHerein, we present the first, one-step, direct synthesis of unsymmetric phosphorotrithioates through a process involving sequential coupling of 1,1-dichloro-,-diethylphosphanamine with thiols and sulfenyl chloride. This method showcases excellent functional group tolerance, substrate compatibility, and mild reaction conditions, offering a streamlined approach for the challenging phosphorotrithioate synthesis. Additionally, the applicability of this method can be extended to the synthesis of mixed phosphoroselenodithioates.
View Article and Find Full Text PDFIn this study, we report a novel and efficient one-pot synthesis of mixed phosphorotrithioates under mild conditions at ambient temperature, obviating the requirement for supplementary additives. The method's versatility stems from its utilization of diverse thiols as nucleophilic reactants, 1-chloro-,,','-tetraisopropylphosphanediamine [bis(diisopropylamino)chlorophosphine] as the phosphorus precursor, and various sulphenyl chlorides as sources of electrophilic sulfur. Notably, our investigation extends beyond mixed phosphorotrithioates to encompass the synthesis of phosphoroselenodithioates, underscoring the broad applicability of this synthetic protocol.
View Article and Find Full Text PDFAn efficient strategy towards stereoselective amidation of alkynes is reported. The given method features operational simplicity, excellent functional group tolerance, broad substrate scope and fast kinetics to furnish -enamides. Moreover, the method was successfully applied for the facile synthesis of the natural products lansiumamide A, lansiumamide B and -alatamide.
View Article and Find Full Text PDFThe ring-opening functionalization strategy in tetrahydrofuran (THF) represents an ideal approach to access different valuable structures. Herein, we report different operationally simple, efficient, unique, and practical regioselective heteronucleophilic ring-opening strategies for the THF system. TfO, which is a strong electrophilic activator, was found to generate a THF triflate intermediate that triggers the nucleophilicity of nitriles (Nu) and led to regioselective ring opening in the presence of different nucleophiles (Nu).
View Article and Find Full Text PDFA simple and efficient protocol for the synthesis of arylmethyl substituted organophosphorus compounds is presented. This method involves the reaction of diphenyl phosphite with aldehydes in the presence of BF-EtO. In this method, BF-EtO plays a dual role, as it facilitates the generation of both hydrophosphonylated intermediate and phenol from diphenyl phosphite.
View Article and Find Full Text PDFThe role of two types of acute physical activity (PA) bouts were assessed on young adults' free-recall and recognition memory in two experiments, which differed in the temporal relation of PA and word encoding. Before or following training on the Rey Auditory Verbal Learning Task, participants performed a simple two-step dance, a complex four-step dance, or remained seated. Hypotheses proposed that PA prior to encoding and complex PA would enhance PA's mnemonic benefits.
View Article and Find Full Text PDFHerein, we present the BF/BF mediated activation of diphenyl phosphite for the formation of thionium ions from aldehydes and thiophenols. These reactive species subsequently undergo reaction with generated phenol, resulting in the synthesis of diarylmethyl thioethers. It was demonstrated that the addition of external phenol in the reaction produced unsymmetrical -diarylmethyl thioethers in good yields.
View Article and Find Full Text PDFAn unprecedented, one-step strategy for the synthesis of 5-(methylthio)pyridazin-3(2)-one derivatives has been developed through iodine triggered deaminative coupling of glycine esters with methyl ketones and hydrazine hydrate in DMSO. These transformations in the absence of hydrazine helped to generate different 3-methylthio-4-oxo-enoates in good yields. Notably, DMSO played multiple roles such as oxidant, methylthiolating reagent, and solvent.
View Article and Find Full Text PDFTranscranial direct current stimulation (tDCS) is a promising technique for enhancement of executive functions in healthy as well as neurologically disturbed patients. However, the evidence regarding the neuropsychological and behavioral change with neurophysiological shifts as well as the mechanism of tDCS action as evidenced by activation of neuronal sources important for executive functions have remained unaddressed. The study thereby endeavors to (1) determine the neuropsychological, behavioral, and neurophysiological change induced with five sessions of bilateral tDCS stimulation and (2) identify putative neuronal sources related to the executive functions responsible for neuropsychological and behavioral change.
View Article and Find Full Text PDFAn efficient strategy towards -formylation of amides and oxidation of indolines to isatins is described. This method employs readily available (NH)SO, I, and DMSO. The given method features operational simplicity, excellent functional group tolerance, broad substrate scope, and fast kinetics.
View Article and Find Full Text PDFA series of novel 1,2,3-triazole derivatives of capsaicin and its structural isomer (new natural product hybrid capsaicinoid) were synthesized by exploiting one-/two-point modification of capsaicin without altering the amide linkage (neck). The newly synthesized compounds were screened for their antiproliferative activity against an NCI panel of 60 cancer cell lines at a single dose of 10 μM. Most of the compounds have demonstrated reduced growth between 55 and 95%, whereas capsaicin () has shown reduced growth between 0 and 24%.
View Article and Find Full Text PDFDescribed herein is a simple, novel, one-pot acylamination reaction of unactivated alcohols. This reaction employs the combination of PCl and triflic anhydride (TfO) or copper triflate Cu(OTf), which serves as a source of P(IV)-activated complex for nitriles to react under the Ritter-type mechanism. The synthetic utility of TfO-promoted reactions was demonstrated by its effectiveness to generate different acylaminated products.
View Article and Find Full Text PDFHerein, we present the first mild, one-step direct synthesis of mixed phosphorothioates through selective generation of O-P(O)-S bonds at rt under additive-free condition. Further, reactions of different model natural products with 1,1-dichloro-,-diisopropylphosphanamine helped to present an alternative dimerization strategy. The synthetic utility of the methodology was extended for the synthesis of mixed phosphoroselenoates as well.
View Article and Find Full Text PDFAn efficient method is described for the preparation of molnupiravir (EIDD-2801) an antiviral agent regioselective conversion of an acyl-nucleoside intermediate, generated through stereo and regioselective glycosylation of protected ribose and -acetyl cytosine, to an amidoxime. This method avoids use of expensive starting materials, enzymes, complex reagents, and cumbersome purification procedures.
View Article and Find Full Text PDFSuspension microsphere immunoassays are rapidly gaining attention in multiplex bioassays. Accurate detection of multiple analytes from a single measurement is critical in modern bioanalysis, which always requires complex encoding systems. In this study, a novel bioassay with Raman-coded antibody supports (polymer microbeads with different Raman signatures) and surface-enhanced Raman scattering (SERS)-coded nanotags (organic thiols on a gold nanoparticle surface with different SERS signatures) was developed as a model fluorescent, label-free, bead-based multiplex immunoassay system.
View Article and Find Full Text PDFBy facilitating the chemical conversion of thiols to thiosulfonates, phosphoramidite/phosphite bearing sp-hybridized carbon serves as an ideal coupling material to forge new connections at room temperature. In this work, a functional group-induced, additive-free, novel, S-P bond-forming approach is presented. This protocol exhibits good functional group tolerance with wide applications that include phosphorylation of cysteine derivatives, development of a one-pot approach to mixed unsymmetrical thiophosphonates, and extension of the concept to different Se-P bonds.
View Article and Find Full Text PDFA highly selective, mild, and efficient method for the cleavage of oxophenylacetyl ester protected saccharides was developed using triethylamine in methanol at room temperature. The reagent proved successful against different labile groups like acetal, ketal, and PMB and also generated good yields of the desired saccharides bearing lipid esters. Further, we also observed DBU in methanol as an alternative reagent for the deprotection of acetyl, benzoyl, and oxophenylacetyl ester groups.
View Article and Find Full Text PDFBouts of exercise performed either prior to or immediately following study periods enhance encoding and learning. Empirical evidence supporting the benefits of interventions that simultaneously pair physical activity with material to be learned is not conclusive, however. A narrative, theory-based review of dual-task experiments evaluated studies in terms of arousal theories, attention theories, cognitive-energetic theories, and entrainment theories.
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