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The pentafluorosulfanyl (SF 5 -) group has been the subject of a surge of interest in the past decade, but there is still little practicality associated with its synthesis and installation. Herein is reported the first continuous flow synthesis of pentafluorosulfanyl chloride (SF 5 Cl), the most common reagent for the synthesis of SF 5 -substituted compounds. The synthesis is based on inexpensive and easy-to-handle reagents: sulfur powder (S 8 ), trichloroisocyanuric acid (TCCA) and potassium fluoride (KF). To this end, a custom-made stirring reactor was designed to allow for fast, safe, and highly efficient on-demand synthesis of SF 5 Cl. The resulting SF 5 Cl solution is showcased in the radical addition on alkynes in a telescoped fashion., (© 2024 The Author(s). Chemistry - A European Journal published by Wiley-VCH GmbH.)

Regioselective C-H difluoroalkylation of diverse 2-pyridones with ethyl bromodifluoroacetates and bromodifluoroacetamides is accomplished by using a (dppf)NiCl 2 catalyst under mild conditions. This efficient protocol could deliver a variety of C-3 difluoroalkylated pyridones with the tolerance of a range of highly susceptible functionalities, such as -Cl, -Br, -I, -COMe, -CN, -NMe 2 and -NO 2 , including heteroarenes like pyridinyl, furanyl, thiophenyl and carbazolyl moieties. A preliminary mechanistic study suggests the radical pathway for the reaction involving fluoroalkyl radical intermediate., (© 2025 Wiley-VCH GmbH.)

Given the profound effect of fluorine‐containing groups in improving the chemical, physical, and biological properties of the parent compound, the fluorine‐containing groups were receiving increasing attention in the medicinal, pharmaceutical, agricultural, and material sciences. Unlike well‐developed trifluoromethylation and difluoromethylation reactions, the efficient and mild methods for rapid introduction of CF2Me are still underdeveloped, despite their important applications in pharmaceuticals and agrochemicals. This concept describes recent progress in difluoroethylation functionalization. [ABSTRACT FROM AUTHOR]

The sulfur‐fluorine partnership occupies a privileged position in fluorine chemistry given the functional versatility that it imparts to organic structures. Despite this, available methodologies to forge S−F bonds are limited compared to C−F bond formation. Here, we describe a synthetic protocol that selectively enables the oxidative halogenation of aliphatic, aromatic, and heteroaromatic thiols to their corresponding SF4Cl, SO2F and SF3 derivatives. Selective oxidation of thiols to either S(IV)‐F or S(VI)‐F compounds is achieved by employing bench‐stable calcium hypochlorite as chlorine surrogate (CLOgen), in the presence of KF as fluoride source. Density functional theory (DFT) calculations provided insight into the mechanistic aspects of the transformation and rationalized the observed isomeric preference towards the SF4Cl derivatives. Ultimately, this glovebox‐free method selectively dispatches three classes of compounds upon reaction condition fine‐tuning. Furthermore, first‐in‐class transformations are reported, including the preparation of aliphatic SF4Cl intermediates, their transformation into aliphatic sulfur pentafluoride analogs, and post‐functionalizations that allow accessing highly complex SF4‐bridged scaffolds. [ABSTRACT FROM AUTHOR]

One or more nitrogen‐containing molecules constitute an important class of heterocyclic compounds in organic synthesis, due to their reactivity and their presence in many molecules of natural, human or plant origin. These nitrogenous heterocycles play an essential role in various scientific domains, whether they are chemical, biological or pharmacological. N‐heterocycles are the privileged source of many research topics developed by several groups of researchers. Thus, different methods have been developed to access these heterocyclic compounds with nitrogenous rings, such as triazolopyrimidines. In this review, a bibliographic study summarizing the pharmacological importance of the triazolo[1,5‐a]pyrimidine ring, the different synthesis routes of these derivatives as well as their reactivity was reported. [ABSTRACT FROM AUTHOR]

Pentafluorosulfanyl (SF5)‐containing compounds and corresponding analogs are a highly valuable class of fluorine‐containing building blocks owing to their unique properties. The reason for that is the set of peculiar and tremendously beneficial characteristics they can impart on molecules once introduced onto them. Despite this, their application in distinct scientific fields remains modest, given the extremely harsh reaction conditions needed to access such compounds. The recent synthetic approaches via S−F, and C−SF5 bond formation as well as the use of SF5‐containing building blocks embody a "stairway‐to‐heaven" loophole in the synthesis of otherwise‐inaccessible chemical scaffolds only a few years ago. Herein, we report and evaluate the properties of the SF5 group and analogs, by summarizing synthetic methodologies available to access them as well as following applications in material science and medicinal chemistry since 2015. [ABSTRACT FROM AUTHOR]

The sulfur-fluorine partnership occupies a privileged position in fluorine chemistry given the functional versatility that it imparts to organic structures. Despite this, available methodologies to forge S-F bonds are limited compared to C-F bond formation. Here, we describe a synthetic protocol that selectively enables the oxidative halogenation of aliphatic, aromatic, and heteroaromatic thiols to their corresponding SF 4 Cl, SO 2 F and SF 3 derivatives. Selective oxidation of thiols to either S(IV)-F or S(VI)-F compounds is achieved by employing bench-stable calcium hypochlorite as chlorine surrogate (CLOgen), in the presence of KF as fluoride source. Density functional theory (DFT) calculations provided insight into the mechanistic aspects of the transformation and rationalized the observed isomeric preference towards the SF 4 Cl derivatives. Ultimately, this glovebox-free method selectively dispatches three classes of compounds upon reaction condition fine-tuning. Furthermore, first-in-class transformations are reported, including the preparation of aliphatic SF 4 Cl intermediates, their transformation into aliphatic sulfur pentafluoride analogs, and post-functionalizations that allow accessing highly complex SF 4 -bridged scaffolds., (© 2023 Wiley-VCH GmbH.)

Malaria is a serious worldwide medical issue that results in substantial annual death and morbidity. The availability of treatment alternatives is limited, and the rise of resistant parasite types has posed a significant challenge to malaria treatment. To prevent a public health disaster, novel antimalarial agents with single-dosage therapies, extensive curative capability, and new mechanisms are urgently needed. There are several approaches to developing antimalarial drugs, ranging from alterations of current drugs to the creation of new compounds with specific targeting abilities. The availability of multiple genomic techniques, as well as recent advancements in parasite biology, provides a varied collection of possible targets for the development of novel treatments. A number of promising pharmacological interference targets have been uncovered in modern times. As a result, our review concentrates on the most current scientific and technical progress in the innovation of new antimalarial medications. The protein kinases, choline transport inhibitors, dihydroorotate dehydrogenase inhibitors, isoprenoid biosynthesis inhibitors, and enzymes involved in the metabolism of lipids and replication of deoxyribonucleic acid, are among the most fascinating antimalarial target proteins presently being investigated. The new cellular targets and drugs which can inhibit malaria and their development techniques are summarised in this study., (© 2023 Naveen Kumar Reddy Chinnappanna et al., published by Sciendo.)

Pentafluorosulfanyl (SF 5 )-containing compounds and corresponding analogs are a highly valuable class of fluorine-containing building blocks owing to their unique properties. The reason for that is the set of peculiar and tremendously beneficial characteristics they can impart on molecules once introduced onto them. Despite this, their application in distinct scientific fields remains modest, given the extremely harsh reaction conditions needed to access such compounds. The recent synthetic approaches via S-F, and C-SF 5 bond formation as well as the use of SF 5 -containing building blocks embody a "stairway-to-heaven" loophole in the synthesis of otherwise-inaccessible chemical scaffolds only a few years ago. Herein, we report and evaluate the properties of the SF 5 group and analogs, by summarizing synthetic methodologies available to access them as well as following applications in material science and medicinal chemistry since 2015., (© 2022 Wiley-VCH GmbH.)