Palladium(II) Complexes of Bis(diphosphene) with the Different Coordination Behavior

Organophosphorus compounds possessing the P−P double-bond character are intriguing materials in coordination chemistry because it is possible to form a variety of coordination modes from the π-bond in addition to...

Nickel/brønsted acid dual-catalyzed regio- and enantioselective hydrophosphinylation of 1,3-dienes: access to chiral allylic phosphine oxides

While chiral allylic organophosphorus compounds are widely utilized in asymmetric catalysis and bioactive molecules, their synthetic methods are still very limited. We report the development of an asymmetric nickel/brønsted acid...

Investigation of the Experimental Pharmacokinetics of the Bis-Chlorinated Bis-pyridinium Mono-aldoxime Cholinesterase Reactivator K-868 in Rats

Background: The widespread use of organophosphorus compounds in agriculture and their existence in some military arsenals present continuous threats. Quaternary bis-pyridinium aldoximes are potent, highly polar cholinesterase reactivators and the most intensively studied candidate antidotes against poisoning with organophosphorus compounds. Objective: The in vivo experimental pharmacokinetic properties of K-868, a novel bis-chlorinated, bis-pyridinium mono-aldoxime are detailed and put in context with regard to similar compounds described earlier. Methods: Rats received 30 µmol K-868 i.m. and were sacrificed at various time points following treatment. Blood, cerebrospinal fluid and tear were collected, while the brains, eyes, kidneys, livers, lungs and testes were removed, dissected and homogenized. K-868 concentrations were determined using high performance liquid chromatography with ultraviolet absorption detection. Results: K-868 was detected in the eyes, kidneys, lungs and tear within 5 minutes in maximal serum concentrations attained 15 minutes following administration. Elimination was slow for K-868 which remained detectable at 120 minutes in the blood and the kidneys, and at 60 minutes in the eyes, lungs and tear following its administration. Nevertheless, its distribution was overall poor with areas under the 120-minute concentration curves (AUC120) showing close similarity in the blood and the kidneys, while reaching just approximately 5% of serum AUC120 in the eyes and lungs. Conclusion: K-868 is a potent candidate antidote against organophosphate poisoining with a prolonged presence in the circulation.

Facile Synthesis of the Dicyanophosphide Anion via Electrochemical Activation of White Phosphorus: An Avenue to Organophosphorus Compounds

Organophosphorus compounds (OPCs) have gained tremendous interest in the past decades due to their wide applications ranging from synthetic chemistry to materials and biological sciences. We describe herein a practical and versatile approach for the transformation of white phosphorus (P4) into useful OPCs with high P atom economy via a key bridging anion [P(CN)2]–. This anion can be prepared on a gram scale directly from P4 through an unprecedented electrochemical process. A variety of OPCs involving phosphinidenes, cyclophosphanes and phospholides have been made readily accessible from P4 in a two-step manner. Our approach has a significant impact on the future preparation of OPCs in laboratory and industrial settings.

Medicines and life (to the 100th anniversary of Professor Irina Vitalievna Zaikonnikova)

Irina Vitalevna Zaikonnikova is a well-known Soviet pharmacologist, headed the Department of Pharmacology of the Kazan State Medical Institute between 1968 and 1989. The topic of I.V. Zaikonnikovas Ph.D. thesis was The influence of dikain on blood vessels and its relationship with adrenaline. In her dissertation, Irina Vitalievna found that dicaine dilates blood vessels in low concentrations and causes their constriction in high concentrations. The thesis was successfully defended in 1947. In the 50s of the last century in Kazan, for the first time in the Soviet Union, the study of the biological activity of organophosphorus compounds was begun. A large experimental material concerning the correlation between the biological activity and chemical structure of compounds was summarized in his doctoral dissertation Pharmacological characteristics of a number of dialkylphosphinic acid esters, which I.V. Zaikonnikova defended in 1968. At the Department of Pharmacology, which she headed since 1968, a close-knit team was formed, united by a common interest the search and development of new potential drugs. This major work resulted in the creation of cidiphos, glycifon, phosphabenzide, and dimephosphon organophosphorus compounds of a new type, which mechanism of action is not associated with inhibition of the activity of acetylcholinesterase. In addition, drugs that did not belong to organophosphates were created the daytime tranquilizer mebikar, a regeneration stimulator with the immunomodulatory effect of xymedon. At present, the Department of Pharmacology of Kazan State Medical University continues the scientific traditions of our outstanding predecessors.

THE PATTERN OF ORGANOPHOSPHORUS COMPOUNDS POISONING AT A TERTIARY CARE TEACHING HOSPITAL AND MEDICAL COLLEGE IN NORTHERN INDIA

Objective: A retrospective study was conducted in a tertiary care hospital collaborated with a medical college, to analyze the drug therapy including antidotes administered and pattern of Organophosphorous compounds poisoning. Material and methods: The data are analytically drawn from record sheets of Organophosphorous poisoning patients. The collected tabulated data were statistically analyzed with SPSS version for the pattern of Organophosphorous compounds poisoning. Results: The demographic data of 122 Organophosphorous poisoning clinical cases documented 84.42 % suicidal tendency and 15.57 % accidental exposure of patients, 66.39 % in the age of 15-24 years, and 70.49 % were females and 70.49 % from a rural background, and 29.50 % from an urban background. Before pharmacotherapy, all patients were subjected to general supportive measures including stomach wash, and patients were administered pharmacotherapy consisting of Pralidoxime (23.77 %) and Atropine (41.80 %). Conclusion: This present concluded that patients diagnosed with Organophosphorous poisoning can be managed by alone administration of atropine as an antidote which is available as a cost-effective drug as compared to Pralidoxime. Thus cost-effectiveness can be significantly reduced by the rational drug use and strict implementation of the pesticide act to further strengthen the proper maintenance of procurement of Organophosphorous compounds for exclusive agricultural purpose.

Unintended Inhalational Organophosphate Poisoning Presenting as Angioedema: A Rare Case Report

Organophosphorus compounds are chemical agents in widespread use throughout the world, mainly in agriculture. In developing countries organophosphorus (OP) poisoning is a commonly encountered problem. Here we present a rare case of OP poisoning with angioedema as the presenting feature. Prompt treatment of these cases will help in reducing the morbidity and mortality.

Electrochemical C–H phosphorylation of arenes in continuous flow suitable for late-stage functionalization

The development of efficient and sustainable methods for carbon-phosphorus bond formation is of great importance due to the wide application of organophosphorus compounds in chemistry, material sciences and biology. Previous C–H phosphorylation reactions under nonelectrochemical or electrochemical conditions require directing groups, transition metal catalysts, or chemical oxidants and suffer from limited scope. Herein we disclose a catalyst- and external oxidant-free, electrochemical C–H phosphorylation reaction of arenes in continuous flow for the synthesis of aryl phosphorus compounds. The C–P bond is formed through the reaction of arenes with anodically generated P-radical cations, a class of reactive intermediates remained unexplored for synthesis despite intensive studies of P-radicals. The high reactivity of the P-radical cations coupled with the mild conditions of the electrosynthesis ensures not only efficient reactions of arenes of diverse electronic properties but also selective late-stage functionalization of complex natural products and bioactive compounds. The synthetic utility of the electrochemical method is further demonstrated by the continuous production of 55.0 grams of one of the phosphonate products.