Реферат: Three groups of amidoxime derivatives: nitrogen derivatives of alfa-chlorine-alfa-izonitrozoacetone, hydrochlorides of O-aroyl-beta-aminopropio-amid-oximes and 3-[beta-(pyperidin-1-yl)]ethyl-5-aryl-1,2,4-oxadiazoles were tested in the conditions of conducting, infiltrating and terminal anaesthesia. In the bulk all tested compounds are active at conducting and infiltrating anaesthesia on the level of standard preparations (trimecainum, lidocaine, novocainum, kazkain); tested compounds doesn\'t show activity at terminal anaesthesia. Compounds VII - X are of interest for extending tests at conducting and infiltrating anaesthesia.
Interaction of the О-Benzoyl-b-aminopropioamidoximes with Lawesson\'s Reagent and Spectral Characterization of the Products
Автор(ы): Каюкова Л. А.*Пралиев К. Д.*Кемельбеков У. С.*Абдильданова А.*Gutyar V.*
Реферат: Interaction of O-benzoyl-beta-aminopropioamidoximes [beta-aminogroup: pyperidin-1-yl; morpholin-1-yl; thiomorpholin-1-yl; 4-phenylpiperazin-1-yl; benzimidazol-1-yl] with Lawesson\'s reagent was done in tetrahydrofuran at heating to 70 grad. C during 10 h. New O-thiobenzoyl-beta-aminopropioamidoximes were obtained with the outputs 57?96 %; they were characterized with the help of physicochemical, IR and NMR spectra.
Organocatalytic asymmetric synthesis of polyfunctionalized 3-(cyclohexenylmethyl)-indoles via a quadruple domino Friedel-Crafts-type/Michael/Michael/Aldol condensation reaction
Реферат: A new organocatalytic quadruple domino Friedel-Crafts-ype/Michael/Michael/aldol condensation reaction has been developed. In this one-pot multi-component process acrolein, various indoles and nitroalkenes are used as starting materials. The diphenylprolinol TMS-ether catalysis provides a straightforward and efficient entry to 3-(cyclohexenylmethyl)-indoles bearing three stereogenic centers in moderate to excellent yields (23-82%) and excellent stereoselectivities (dr = 91: 9 to >95: 5, ee = 94 to >99%).
Crystal structure of [3,5-dimethyl-4-(prop-2-ynyl)-1Hpyrazol-1-yl](2-furyl)methanone, C13H12N2O2
Автор(ы): Beketov K. М.*Vizer S.*Yerzhanov K. K.*
Объем документа: P. 569-570
МРНТИ: 31.21.01
Ключевые слова: crystal structure*pyrazol*
Реферат: C13H12N2O2, monoclinic, P121/c1 (no. 14), a = 7.928(2) Е, b = 16.358(3) Е, c = 9.506(2) Е, * = 106.44(3)grad., V = 1182.4 Е3, Z = 4, Rgt(F) = 0.064, wRref(F2) = 0.209, T = 293 K.
New Catalysts Based on the Heteropoly Acid-Zeolite System for the Synthesis of Higher alff-Olefins by Paraffin Cracking
Автор(ы): Кадирбеков К. А.*Конуспаев С. Р.*Нурбаева Р. К.*Сарсекова А. Т.*
Реферат: Abstract-Natural zeolites (clinoptilolite) from the Shankanay deposit in Almaty oblast were used to prepare catalysts for the synthesis of higher alfa_olefins by paraffin cracking. The modification of zeolite with inorganic and organic heteropoly acids resulted in an enhancement of catalytic activity. The olefin yield on the zeolite modified with heteropoly acids was as high as 36.6% after one run in a flow system at atmospheric pressure and temperatures of 500-525 grad C. The modification of natural zeolite with HPA led to an increase of 22 to 257 m2/g in the total surface area. The increase in catalytic activity after HPA deposition can be attributed to the formation of stable nanostructures with sizes of 1 to 4 nm, resulting in the emergence of stronger Brinsted acid sites. The catalyst works stably in the reaction-regeneration mode.
Реферат: При кислотном гидролизе ряда 5-арил 3-(b-тиоморфолино)этил- -1,2,4-оксадиазолов в каждом случае получены замещенные бензойные кислоты и гидрат 2-амино-8-тиа-1-aзa-5-aзониаспиро[4.5]дек-1-eн хлорид, структура которого доказана физико-химическими и спектральными методами и РСА.
Rapid acid hydrolysis of 5-aryl-3-(b-thiomorpholinoethyl)-1,2,4-oxadiazoles
Автор(ы): Kayukova L. A.*Orazbaeva M. A.*Gapparova G. I.*Beketov K. M.*Espenbetov A. A.*Faskhutdinov M. F.*Tashkhodjaev B. T.*
Реферат: The acid hydrolysis of a series of 5-aryl-3-(?-thiomorpholinoethyl)-1,2,4-oxadiazoles gave substituted benzoic acids and 2-amino-8-thia-1-aza-5-azoniaspiro[4.5]dec-1-ene chloride hydrate, whose structure was demonstrated by spectral methods and X-ray diffraction structural analysis.
Синтез и противотуберкулезная активность О-ароил-b-(4-фенилпипера-зин-1-ил)пропиоамидоксимов
Автор(ы): Каюкова Л. А.*Оразбаева М. А.*Бисмильда В. Л.*Чингисова Л. Т.*
Объем документа: С. 356-359
МРНТИ: 31.21.27
Ключевые слова: туберкулостатики*противотуберкулезная активность*замедленная инверсия гетероцикла*штаммы M. tuberculosis*
Реферат: Поиск новых туберкулостатиков - важная задача для химиков, работающих в области медицинской химии. Был синтезирован ряд новых O-ароил-b-(4-фенилпиперазин-1-ил)пропио-амидоксимов и тестирован на in vitro противотуберкулезную активность. Синтез целевых соединений состоит из 3 - 4 стадий. Первая стадия заключается в получении b-(4-фенилпиперазин-1-ил))пропионитрила с выходом 79 %; вторая стадия - синтез b-(4-фенил-пиперазин-1-ил)пропиоамидоксима с выходом 75 %. При ароилировании b-(4-фенил-пиперазин-1-ил)пропиоамидоксима хлорангидридами замещенных бензойных кислот в присутствии триэтиламина с выходами 61 - 93 % выделены O-ароил-b-(4-фенил-пиперазин-1-ил)-пропиоамидоксимы. Гидрохлориды О-ароилированных продуктов были получены с выходами 72 - 94 % действием эфирного раствора НСl на растворы оснований. 1Н ЯМР спектры гидрохлоридов продуктов О-ароилирования указывают на замедленную инверсию гетероцикла в b-положении и на координацию молекулы HCl у атома N1 4-фенилпиперазинового фрагмента. Некоторые из оснований и гидрохлоридов O-ароил-b-(4-фенил-пиперазин-1-ил)пропиоамидоксимов имеют интересные in vitro противотуберкулезные свойства на чувствительных, устойчивых и многолекарственноустойчивых штаммах M. tuberculosis.
Synthesis and antituberculosis activity of O-aroyl-b-(4-phenylpiperazin-1-yl)propioamidoximes
Автор(ы): Kayukova L. A.*Orazbaeva M. A.*Bismilda V. L.*Chingisova L. T.*
Объем документа: P. 356-359
МРНТИ: 31.21.27
Ключевые слова: туберкулостатики*противотуберкулезная активность*замедленная инверсия гетероцикла*штаммы M. tuberculosis*
Реферат: The search for new tuberculostatics is an important task for medicinal chemistry. A series of new O-aroyl-b-(4-phenylpiperazin-1-yl)propioamidoximes were synthesized and tested in vitro for antituberculosis activity. The synthesis of the target substances consists of 3 - 4 steps. In the first step, b-(4-phenylpiperazin1-yl)propionitrile was obtained in 79% yield; the second step yields b-(4-phenylpiperazin-1-yl)propioamidoxime in 75% yield. Subsequent aroylation of this amidoxime by substituted benzoic acid chlorides in the presence of Et3N leads to the target O-aroyl-b-(4-phenylpiperazin-1-yl)propioamidoximes in 61 - 93% yields. Hydrochlorides of the O-aroylated products were obtained in 72 - 94% yields by the action of ethereal HCl on solutions of the bases. PMR spectra of hydrochlorides of the O-aroylated products show evidence of slow inversion of the heterocycle at the b-position and coordination of HCl at the N1 atom of the 4-phenylpiperazine fragment. Some bases and hydrochlorides of O-aroyl-b-(4-phenylpiperazin-1-yl)propioamidoximes exhibited interesting antituberculosis properties when tested in vitro on sensitive, resistant, and multi-drug resistant strains of M. tuberculosis.
Study of Quinoid Derivatives of Allylamine Polymerization
Автор(ы): Ergozhin E. E.*Mukhitdinova B. A.*Nikitina A. I.*Razuvaeva N. I.*
Реферат: We have studied radical and cationic initiation of monomers on the basis of quinoid derivatives of allylamine by the method of polarography, and developed optimum conditions of synthesis of polymers, and studied their structure and the basic properties.
