A novel sequential one-pot bimetallic catalytic system combining Fe(III)-catalyzed alkynylation and a Rh(I)-catalyzed [2+2+2] reaction was successfully developed. The σ-Lewis acid properties of iron (III) and the π-Lewis acid properties of rhodium (I) catalysts were unified in an unprecedented intermolecular alkynylation/cyclotrimerization one-pot process. Using this unique Fe/Rh bimetallic relay catalytic system, a variety of benzo and pyrridinoisoindolinone derivatives were obtained under mild conditions from easily available N-(propargyl) hydroxy aminals, as the simplest N-acyliminium ion precursors, and several alkynes.

Introduction The present study focuses on the development of doped phosphate catalysts for the green synthesis of functional amidines. Methods The natural phosphate was characterized by XRF, FTIR-IR, and XRD, while the calcined natural phosphate doped with zinc was analyzed using XRD, FTIR-IR, and EDX. Furthermore, the amidines were characterized using 1H and 13C NMR spectroscopy, as well as HRMS analysis. Results This phosphate catalyst is recyclable and retains its catalytic efficiency over multiple uses. Under optimized conditions, a series of amidines were obtained in high yields up to 95% at room temperature and atmospheric pressure. Discussion The XRD spectrum of the natural phosphate revealed characteristic peaks of hydroxyapatite, fluorapatite, and carbonate apatite, along with secondary phases, such as quartz, vermiculite, and nacrite. In the zinc-doped material, additional peaks corresponding to zinc oxide and skorpionite were observed, alongside the original ones. These findings indicate that the primary apatite structure remains intact after doping and calcination, while the appearance of zinc-containing phases suggests that zinc is not incorporated into the apatite lattice, but rather forms separate crystalline phases. Conclusion This study presents a straightforward and green process for synthesizing amidines by reacting N-Boc thioacetamide with various amino esters, using calcined natural phosphate doped by zinc as a heterogeneous catalyst.

I N MAURITANIA, herbal medicine is an integral part of the culture of the society. However, ethno-medicinal data remain scarce and fragmentary. In this work, the ethno-medicinal knowledge in five regions inhabited mainly by two Mauritanian ethnic groups: the "Maures" and the "Peulhs" was explored. These regions present the climatic stages of the country from hyper-arid to SaheloSaharan. This suggests that the use of plants by the population in their health care will depend on their presence in the environment. Our methodology consists of a diagnosis of the current situation of this herbal medicine through an ethno-medical survey of healers in the regions of Tiris Zemmour, Inchiri, Adrar (North), Trarza and Brakna (South West). seventy-six informants were enrolled in this study. Results showed that (93.42%) of the informants belong to the 'Maures' community and that women (64.45%) are more involved in this practice The majority of traditional healers are married (97.38%). The older people and the least educated are the most present in the profession. The ethnobotanical study made it possible to inventory 56 medicinal species, used in phytotherapy, belonging to 25 families. The most cited are Ziziphus lotus, Ziziphus mauritiana, Vachellia tortilis, Adansonia digitata, Gymnosporia senegalensis, and Senegalia senegal. The modes of administration exhibit that the aerial part is the most used (53.50%). The majority of remedies are prepared as infusions (48%) and maceration (22%). The majority of medicines are administered orally (99.77%). Most of medicinal species in the five regions studied are prescribed for diseases of the digestive tract (53.50%). No difference has been observed in the use of this medicine among ethnic groups. these data will serve as a basis for researchers and as a reference for establishing action plans for the conservation of Mauritanian flora in general and traditional medicine in particular.

Many efforts have been made recently to develop solutions to corrosion problems. The current study was focused on synthesizing a new epoxy compound called Tetraglycidyl orthophenyl diamine (TGOPDA) and using it as a powerful inhibitor of carbon steel C38 in 1 M HCl for the first time. Furthermore, the title molecule’s structure was discovered utilizing Fourier transform infrared spectroscopy. The corrosion inhibition and adsorption behavior of TGOPDA onto C38 surface was then evaluated in 1 M HCl utilizing the weight loss measurements, thermodynamic/kinetic parameters and electrochemical techniques (Open circuit potential), Potentiodynamic polarization (PDP) and Electrochemical impedance spectroscopy (EIS)). Additionally, surface morphology (SEM/EDX) with computational tools such as: DFT (Density functional theory) calculations, RDF (Radial distribution function) analysis, MC (Monte Carlo) and MD (Molecular dynamic) simulations were combined to get insights into our inhibitor adsorption on C38 steel surface. The EIS tests demonstrated that the addition of TGOPDA improved the effectiveness of C38 steel inhibition, reaching about 95.27

The inhibitory effect of the methanol extract of Grewia bicolor fuss (GB) leaves against XC48 mild steel corrosion, in hydrochloric acid solution (1M) medium, was investigated by potentiodynamic polarization, and electrochemical impedance spectroscopy (EIS) methods for different concentrations at 298 K and weight loss measurements with optimum concentration at different temperatures (298-333 K) and time immersion. The results demonstrated that the components of the extract took action mainly as a mixed -type inhibitor, and the inhibition efficiency values escalated with the progression of extract concentration. The maximum value obtained is about 93% at a concentration of 1500 ppm. This high efficiency can be attributed to the installation of a protecting blanket on the electrode surface. The adsorption of the inhibitor molecules on adsorbate surface obeyed Langmuir isotherm model. The thermodynamic parameter values suggested that physisorption and chemisorption constituted the major contribution to the process of adsorption. Results obtained from weight loss measurements show that the inhibition efficiency decreases with increasing immersion time and temperature. Finally, scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) analyses confirmed obtained results, which reveal that adsorbed inhibitor molecules hinder HCl attacks at the steel grain boundaries.

The inhibitive effect of a methanol extract of Grewia bicolor Juss (Gbj) leaves on the corrosion of XC48 steel in 0.5 M H2SO4 solution has been evaluated by weight loss measurement as well as potentiodynamic polarization (PDP), electrochemical impedance spectroscopy (EIS) and surface characterization techniques. The presence of this extract brings down remarkably the corrosion rate of XC48 steel in 0.5 M H2SO4 solution. The results from this corrosion test clearly showed that the extract behaves as a mixed type corrosion inhibitor with the highest inhibition at 1500 ppm. The effect of temperature on the corrosion behavior of XC48 steel was studied in the range of 298-333 K. The activation and free energy values of the inhibition reaction support the hypothesis of a/the physisorption mechanism well described by the Langmuir equilibrium mode. Scanning electron microscopic (SEM) observations showed that the Gbj extract forms a protective layer over the metallic surface that isolates the metal from aggressive acid solution and protects it against corrosive dissolution. Finally, results of FTIR analysis indicate that the important role played by the oxygen atoms and aromatic rings in the process of adsorption.

Palm (Phoenix dactylifera L.) is a specie cultivated in Mauritania. The present study is focused on the potential of the aqueous extract of the Pergularia tomentosa L., as biological control agent against Fusarium brachygibbosum, the main agent of the date palm stipe rot disease in Mauritania. Fungal pathogen was isolated from symptomatic date palm stipe rot disease in Mauritania. The morphological characterization and the molecular identification by sequencing ITS1, ITS2 5.8 RNAr region showed homology of 98% with Fusarium brachygibbosum strain UOA/ HCPF 16982 s during in vitro tests on leaves performed to verify its phytopathogenicity. The inhibitory effect of aqueous extract of Pergularia tomentosa L. on the phytopathogenic isolate (Fusarium brachygibbosum) of date palm, on mycelial growth and spore germination was observed. In fact, in vitro on PDA, mycelial growth ranged from 39.23 to 67.7%, depending on the concentration of the aqueous extract of P. tomentosa. The aqueous extract showed a reduction of spore germination varying from 5.3 to 23.8%. The minimum inhibitory concentrations varied from 1 to 100 mg/ml. The various extracts give high antioxidant activities exhibited by DPPH assay. Multi -variant analysis by PCA plot and the heatmap were done, to evaluate the correlation between the tested parameters. These results suggest the use of Pergularia tomentosa L., extract as a biological agent to control and reduce dam-age caused by Fusarium brachygibbosum.

This article reports a practical synthesis of tert-butyl acetyl-carbamate, C7H13NO3, from N-Boc-thio-acetamide and the study of its crystal structure. The reaction proceeds in the presence of natural phosphate as a catalyst, with excellent yield, simple workup and benign environment. The crystal structure was refined using a transferred multipolar atom model. In the crystal, symmetrical pairs of strong N-H⋯O hydrogen bonds connect the mol-ecules into dimers with an R 2 2(8) ring motif. The inter-actions between neighbouring dimers are mostly van der Waals, between hydro-phobic methyl groups. Hirshfeld surface analysis shows the major contributions to the crystal packing are from H⋯H (42.6%) and O⋯H (26.7%) contacts.

Iron-based catalysts were applied in cascade-type reactions for the synthesis of different carbonyl compounds. The reactions proceeded by a new iron-catalyzed cascade of alkynylation/hydration by using both the sigma- and pi-Lewis acid properties of iron salts. The alkynylation reactions of several endo and exocyclic acetoxylactams were achieved with three different catalysts including FeCl3 . 6H(2)O, FeCl3, and Fe(OTf)(3) showing the efficiency of sigma-Lewis acidity of iron (III) salts in catalyzing the alkynylation reaction. We also demonstrated that the reaction sequence could be shortened by the direct use of hydroxylactams, leading to an environmentally friendly protocol, avoiding the need to perform unnecessary lengthy steps. A combination of the hard/soft iron Lewis acid properties was then used to implement an unprecedented tandem intermolecular alkynylation/intramolecular hydration sequence allowing expedient access to a new carbonyl structures from trivial materials.

We have recently developed a one-pot process for simultaneous extraction and chemical modification (SECheM) on Cienfuegosia digitata, a Mauritanian Malvaceae called locally "Izide". On the basis of this innovative methodology that consisted of using ground plant roots as starting material in gossypol Schiff base semisynthesis, we now report how this concept can be used to access enantiomerically pure Schiff base atropisomer derivatives of gossypol in only two steps. This study has been envisioned since enantiomerically pure Schiff base atropisomer derivatives of gossypol are generally more potent biologically when compared to racemic gossypol Schiff bases.

INTRODUCTION:Gossypol is an axially chiral natural polyphenol classically extracted from the Malavaceae family. Nevertheless, its extraction and isolation from a plant can be quite complicated and extremely time-consuming since gossypol is known to be sensitive to degradation under solvents, high temperature and light action. Moreover, its purification over column chromatography is a challenging problem due to its ability to oxidise and the existence of various tautomer forms.OBJECTIVE:To develop an efficient "one-step" strategy for simultaneous extraction and semi-synthesis by short-circuiting critical gossypol isolation and purification steps.METHODOLOGY:Gossypol was first isolated from Cienfuegosia digitata roots, characterised (by 1D and 2D NMR) and quantified (by UV spectrophotometry). Thus, aniline was selected to test the "one-step" in situ trapping of freshly extracted gossypol leading to a Schiff base analogue. After screening solvents and extraction times on this model reaction, the "SECheM" (simultaneous extraction and chemical modification) concept was successfully extended to other amines, underlining the efficiency and the robustness of the strategy.RESULTS:After having shown that gossypol occurred as a major compound in C. digitata roots, different experimental procedures using Soxhlet extraction in the presence of aniline pointed out the best conditions for the SECheM concept (7 h of reaction and extraction time in ether as solvent). Ultimately, the concept has been generalised to 17 other amines.CONCLUSION:This is a report of the first semi-synthesis that allows: (1) "in situ" preparation of more stable gossypol Schiff base derivatives directly from ground plant material and (2) circumvention of gossypol extraction and purification problems. Copyright © 2017 John Wiley & Sons, Ltd.

The title compound crys tallizes in the triclinic system, space group P - 1. The parameters of the unit cell are: a = 10.092(7) A, b = 10.956(4) A, c = 12.000(5) A, α = 84.19(3)°, β = 66.97(5)°, γ = 80.80(5)°, Z = 2 and D x = 1.19. The molecular structure shows a benzyl group and two ramified carbon atoms linked to a tertiary nitrogen atom. One ramified carbon has an ethyl group and an ethyl carboxylate group. The other carbon has also a carboxylate group and a carbon linked to a phenyl and a chlore .

AbstractA simple route to new 1,2‐diamines from β‐chloro amines and their transformation into polysubstituted piperazinones are reported.

A practical synthesis of 1,2-diamines from -chloro amines is reported. The reaction proceeds through the intermediacy of an aziridinium ion opening by amines. The conversion of these diamines into polysubstituted piperazinones is also investigated. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications (R) to view the free supplemental file.

New functional dehydrophenylalanines 3 were prepared from β-amino alcohols 1 in a two-step reaction sequence. The synthesis involved chlorination of the starting amino alcohols 1 to afford the intermediate erythro β-chloroamines 2. Treatment of the latter with an appropriate base led to a highly stereoselective elimination reaction, giving the corresponding (E)-dehydrophenylalanine derivatives 3 in high yields. © 2011 Wiley Periodicals, Inc. Heteroatom Chem 23:91–98, 2012; View this article online at wileyonlinelibrary.com. DOI 10.1002/hc.20756

AbstractFor the presented reaction the position of the compounds is limited to the N‐terminus of a peptide chain.

Abstract A series of new trans-N-alkylaziridine-2-carboxylates 3 was conveniently synthesized in a one-pot reaction by treatment of 1,2-amino alcohol mono and diesters 1 with methanesulfonyl chloride in the presence of (iPr)2NEt. The products were obtained in good to excellent yields with high trans-selectivity.

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A variety of 1,2-amino alcohol diesters 1 reacted smoothly with diethyl chlorophosphate under basic conditions to afford the corresponding 1,2-amino phosphate diesters 2 in excellent yields. These compounds served as useful precursors for subsequent nucleophilic attack by alcohols in an SN2 fashion to provide 1,2-amino ether diesters 3.

In the presence of a catalytic amount of amino acid hydrochloride, trans-beta-phenylglycidic ester undergoes ring opening with high stereo- and regioselectivity when treated with glycine esters. Alkylation of the resulting beta-amino-alpha-hydroxy diesters with benzyl bromide, followed by cyclization to furnish the expected 1,4-oxazin-2-ones, is also described.