scholarly journals Palladium-Catalyzed C–H Arylation of Benzofurans with Triarylantimony Difluorides for the Synthesis of 2-Arylbenzofurans

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 97
Author(s):  
Yuki Kitamura ◽  
Yuki Murata ◽  
Mizuki Iwai ◽  
Mio Matsumura ◽  
Shuji Yasuike

Pd-catalyzed regioselective C–H arylation is a useful tool for the chemical modification of aromatic heterocycles and 2-arylbenzofuran derivatives are of interest as biologically active substances. Herein, the reaction of triarylantimony difluorides with benzofurans under aerobic conditions in 1,2-DCE, using 5 mol% Pd (OAc)2 and 2 eq. of CuCl2 at 80 °C, produced a variety of 2-arylbenzofurans in moderate-to-high yields. The reaction is sensitive to the electronic nature of the substituents on the benzene ring of the triarylantimony difluorides: an electron-donating group showed higher reactivity than an electron-withdrawing group. Single crystal X-ray analysis of tri(p-methylphenyl) antimony difluoride revealed that the central antimony atom exhibits trigonal bipyramidal geometry.

2008 ◽  
Vol 47-50 ◽  
pp. 1286-1289 ◽  
Author(s):  
Michael Ioelovich ◽  
Oleg Figovsky

Main purpose of this paper is to describe the method for preparation of the reactive nanocellulose biocarrier and to discuss some its biomedical and cosmetic applications. The method for preparation of the biocarrier was proposed that includes steps of controlled depolymerization of initial cellulose; structural and chemical modification in order to graft various biologically active substances to cellulose particles and high-power mechanical disintegration of the modified cellulose particles in liquid media. As a result, the dispersion of the bioactive nano-cellulose was obtained. Due to nano-size, particles of bioactive nano-cellulose capable clean skin's pores, open them and penetrate through the lipid layer and epidermis within the skin strata. This effect of the biocarrier can be employed at the development of advanced types of biomedical and cosmetics remedies used for gentle care and effective treatment of the skin.


2021 ◽  
Vol 100 ◽  
pp. 05010
Author(s):  
Oleksandr Zabolotnyi ◽  
Larysa Rozborska ◽  
Iryna Leontiuk ◽  
Ivan Zhilyak ◽  
Anna Datsenko

The article deals with the study of the effect of the application of the herbicide Granstar Gold 75, w.g. (water-soluble granulate) and plant growth regulator Regoplant on some ecological indicators of ecocenosis of winter wheat sowing (lipid peroxidation reactions in winter wheat plants by the activity of malonic dialdehyde content accumulation, enzymatic activity, total number of rhizosphere bacteria and anatomical structure of winter wheat leaves). The choice of research topic is due to the fact that currently obtaining high yields of winter wheat is closely connected to the widespread use of chemicals, in particular, herbicides, which by their nature are physiologically active substances that can affect both plants and soil microbiota. This, in turn, leads to the search for environmentally safe elements of technologies for growing winter wheat. One such element may be the use of herbicides together with plant growth regulators. The obtained experimental data testify to the protective ability of the growth regulator Regoplant against the winter wheat plants, as evidenced by a decrease in the activity of malonic dialdehyde accumulation, changes in the activity of the enzymatic defense system, decrease the number of epidermis cells and an increase in total rhizosphere bacteria in case of Regoplant use together with Granstar Gold 75, w.g. compared with the experiment variants, where the herbicide was applied without a growth regulator. That is, the use of growth regulator in a mixture with herbicide to some extent eliminates the toxic effect of xenobiotics, which has a positive effect on the state of ecobiosis of winter wheat sowing.


2019 ◽  
Vol 19 (6) ◽  
pp. 3447-3458 ◽  
Author(s):  
Mahdieh Haghighat ◽  
Farhad Shirini ◽  
Mostafa Golshekan

Immobilized NaHSO4 on core/shell phenylene bridged periodic mesoporous organosilica magnetic nanoparticles (Fe3O4@Ph-PMO-NaHSO4) as a new acidic magnetically separable nanocatalyst was successfully prepared in three steps: (i) preparation of Fe3O4 nanoparticles by a precipitation method, (ii) synthesis of an organic–inorganic periodic mesoporous organosilica structure with phenyl groups on the surface of Fe3O4 magnetic nanoparticles (MNPs) and (iii) finally adsorption of NaHSO4 on periodic mesoporous organosilica (PMO) network. The prepared organic–inorganic magnetic reagent was characterized by Fourier transform infrared spectroscopy (FT-IR), X-ray powder diffraction (XRD), transmission electron microscopy (TEM), N2 adsorption–desorption and energy-dispersive X-ray (EDX) techniques. Finally, it was used as a reusable and new catalyst to promote the synthesis of tetrahydrobenzo[b]pyran and pyrano[2,3-d]pyrimidinone derivatives as important biologically active compounds. Eco-friendly protocol, high yields, short reaction times and easy and quick isolation of the products are the main advantages of this procedure.


Author(s):  
S. Shilin ◽  
Z. Voitenko ◽  
M. Nechai

This paper reports on the synthesis of new derivatives of ε-aminocaproic and γ-aminobutyric acid modified with a pyridin-2-yl substituent at the ω-position of the main chain. The hemostatic activity of both ε-aminocaproic acid itself and its various synthetic analogues is widely known. Likewise, numerous γ-aminobutyric acid derivatives are strong neurotransmitters extensively used in the treatment of the nervous system disorders. No less popular are biologically active substances containing a pyridine or piperidine fragment; among which there are antibiotics, antimalarial, anti-sclerotic and antiallergic drugs, as well as anti-depressants and analgesics. Therefore, the introduction of the pyridine fragment into the amino acid structures is interesting in terms of their potential biological activity investigation. So, a method for the synthesis of 5-amino-5-(pyridin-2-yl)pentanoic and 6-amino-6-(pyridin-2-yl)hexanoic acid has been developed by us. The proposed scheme is based on the available reagents using. The key stage is the Schmidt rearrangement of 2-(pyridin-2-yl)cyclopentanone and 2-(pyridin-2-yl)cyclohexanone, previously synthesized from pyridine N-oxide and cycloalkenyl morpholinide. For synthesized pyridine substituted cycloalkanones according to NMR spectroscopy, the presence of keto-enol tautomerism was established. As a result of Schmidt rearrangement, lactams (2-(pyridin-2-yl)piperidone and 2-(pyridin-2-yl)azepanone) are formed, and the last ones had been hydrolyzed in an acidic medium to open the lactam cycle. Thus, 5-amino-5-(pyridin-2-yl)pentanoic and 6-amino-6-(pyridin-2-yl)hexanoic acid were isolated as hydrochlorides and the hydrochlorides were converted to the zwitterion form using propylene oxide. The first stage of the developed scheme (preparation of pyridylalkanones) occurs in rather low yields, about 35 %. But, after the rearrangement, hydrolysis and the formation of zwitterion do not cause difficulties and are characterized by high yields. Consequently, the proposed synthetic sequence is preparatively advantageous.


Author(s):  
Irina Vyacheslavovna Sergeeva ◽  
Natalya Nikolaevna Gusakova ◽  
Yulia Mikhailovna Andryanova ◽  
Yulia Mikhailovna Mokhonko

The use of synthetic biologically active substances in the technology of cultivation of spring wheat contributes to an increase in its productivity, stable, high yields, and, consequently, to   a sustainable and effective development of agriculture. In the course of our research, we studied the effect of pre-sowing seed treatment with selenium-containing biologically active substances with varying agrophones on the production process of spring wheat in the conditions of leached chernozems of the Saratov Right Bank. The stimulating effect of biologically active substances (selenochromylium perchlorate   and selenochromene) on the sowing qualities of spring wheat (Belyanka and Prokhorovka varieties) was established. A significant increase in the yield of the studied varieties of soft spring wheat was  during inoculation of seeds with solutions of selenochromylium perchlorate   and selenochromene. The application  of biologically active substances, especially selenium-containing substances, increased the payback of mineral fertilizers with an additional harvest. The selenochromene  preparation on the crops of the Prokhorovka variety was the most effective. It is shown that the application  of biologically active substances is an effective way to increase the productivity of agricultural crops.


2017 ◽  
pp. 5-14
Author(s):  
Ольга (Ol'ga) Николаевна (Nikolaevna) Змеева (Zmeeva) ◽  
Наталья (Natal'ja) Эдуардовна (Eduardovna) Коломиец (Kolomiets) ◽  
Наталья (Natal'ja) Юрьевна (Yur'evna) Абрамец (Abramets) ◽  
Руслан (Ruslan) Анатольевич (Anatol'evich) Бондарчук (Bondarchuk)

These materials contain an overview of the most significant publications on the hare (Lotus corniculatus L.) – one of the species of the genus Lotus L., widespread in the territory of the Russian Federation, both in the wild and in culture. The prospect of Lotus corniculatus is confirmed by information about its extensive range of information about the use in the folk medicine of many countries, veterinary science, resistance to disease, the ability to grow and give high yields on different types of soils, high fodder value and melliferous value. Chemical composition of wild and cultivated of Lotus corniculatus was studied in detail. The horned lamb is a rich source of biologically active substances: proteins, polysaccharides, alkaloids, steroids, phytoalexins, saponins, tannins, flavonoids, isoflavones, phenolcarbonic acids, derivatives of anthracene, macro - and micronutrients. The diverse chemical composition of the lapwing explains the wide range of its pharmacological activity (antimicrobial, antifungal, anti-inflammatory, antiparasitic, wound-healing, antiproliferative), use in agriculture, folk medicine, veterinary medicine, cosmetology, and also substantiates the perspectivity of the species for further scientific and practical phytochemical and pharmacological research.


Molbank ◽  
10.3390/m1125 ◽  
2020 ◽  
Vol 2020 (2) ◽  
pp. M1125
Author(s):  
Yuichiro Kanno ◽  
Taichi Kusakabe ◽  
Nao Saito ◽  
Shoko Kikkawa ◽  
Keisuke Takahashi ◽  
...  

The palladium catalyzed carbonylation of 1 using the chiral ligand L1 afforded 2 in a highly diastereoselective manner. The stereochemistry of the major diastereomer 2a was determined by X-ray crystallographic analysis. AR luciferase reporter assay studies suggested that 2a was the active constituent of YK11 (2).


2014 ◽  
Vol 92 (9) ◽  
pp. 888-895 ◽  
Author(s):  
Mohammed Abdul Raheem ◽  
Michael Edmunds ◽  
William Tam

The effect of ethyl and methoxycarbonyl substitution on the C1 position of oxabenzonorbornadienes undergoing palladium-catalyzed nucleophilic ring opening was investigated with a variety of aryl iodide nucleophiles. Electron-withdrawing groups in the C1 position or on the aryl iodide afforded lower yields and led to aromatization of products. The presence of an electron-donating group in either position provided high yields in all cases. Despite variances in electronic nature, all trials produced a single regioisomeric product resulting from addition of the aryl group to the olefin carbon farthest from the C1 substituent. Based on these findings, a mechanism has also been proposed.


2020 ◽  
pp. 43-47

The oxadiazole derivatives complex compounds with metals are biologically active substances. The aim of the study was to study the interaction of the chlorides of Co (II), Ni (II), Cu (II) and Mn (II) with 5-(4-pyridyl)-1,3,4-oxadiazole-2(3H)–thione, ammonium vanadate. Competitive coordination of donor centers, electronic and geometric structures of the ligand molecule were studied on the basis of the quantum-chemical software package Gaussian09 LanL2DZ. It was shown that 5-(4-pyridyl)-1,3,4-oxadiazole-2(3H)-thione ligand is partially coordinated through a localized nitrogen or sulfur atoms at formation of the complex. А procedure was developed for the synthesis of new mixed-metal complexes. The composition and structure of the synthesized compounds were studied using elemental analysis, termogravimetric and X-ray phase analysis and IR spectroscopy.


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