- Rapid access to novel 2-alkylthiopyrimidine derivatives and attempt of their Tacrine analogs synthesis
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A variety of novel 2-alkylthiopyrimidines were synthesized through simple condensation of arylidenemalononitriles with different 2-alkylthiouronium halide derivatives catalyzed by anhydrous potassium carbonate (K2CO3). The reactions have been carried out under mild conditions in i-PrOH, and the products were obtained in moderate to good yields with a simple work-up method. Subsequently, some examples of these compounds have been converted into Tacrine analogs by applying the Friedl?nder reaction.
- Derabli, Chamseddine,Boulcina, Raouf,Kirsch, Gilbert,Debache, Abdelmadjid
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- Having a spiro ring substituent of aryl morpholine compound, its preparation and use
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The invention discloses arylmorpholine compounds with spiro substituents. The arylmorpholine compounds are compounds having the following general formula (I), wherein X is N or CH; R1 is hydrogen, hydroxyl, alkoxy, halogen, amino, amido, acylamino, sulfam
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Paragraph 0167-0169
(2017/08/02)
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- Convenient and environment-friendly synthesis of sulfonyl chlorides from S -alkylisothiourea salts via N-chlorosuccinimide chlorosulfonation
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A convenient, practical, and environmentally friendly method for the synthesis of sulfonyl chlorides has been developed. Structurally diverse sulfonyl chlorides were synthesized in moderate to excellent yields from S-alkylisothiourea salts, which can be easily prepared from readily accessible alkyl halides or mesylates and inexpensive thiourea, via N-chlorosuccinimide chlorosulfonation. In large-scale syntheses, the byproduct succinimide from 'waste water' can be conveniently converted into the starting reagent N-chlorosuccinimide with sodium hypochlorite (bleach) to make the method sustainable. Georg Thieme Verlag Stuttgart, New York.
- Yang, Zhanhui,Xu, Jiaxi
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p. 1675 - 1682
(2013/07/27)
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- ANTIVIRAL PYRIMIDINES
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Disclosed herein are novel compounds comprising substituted pyrimidines, pyrazolopyrimtdines, and imidazolopyrimidines, the syntheses thereof, and compositions thereof, including pharmaceutical compositions, comprising the novel pyrimidines, pyrazolopyrimtdines, imidazolpyrimidines and related compounds. Such compounds function to inhibit entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.
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Page/Page column 78
(2010/11/03)
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- EFFECT OF VICINAL SUBSTITUENTS ON THE REACTIVITY IN BIMOLECULAR NUCLEOPHILIC SUBSTITUTION AT A SATURATED CARBON ATOM. TWO TYPES OF SUBSTITUENTS II. KINETICS OF THE REACTION OF THIOUREA WITH β-SUBSTITUTED BROMOETHANES IN ETHANOL
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The kinetics of the reaction of thiourea with β-substituted bromoethanes in ethanol were studied by radiochromatography.The rate constants and activation parameters of the reactions were determined.It was shown that an isokinetic relationship is observed for the two types of substituents.The mechanisms of the effect of the vicinal substituents on the reactivity are discussed.
- Ryazantsev, G. B.,Shaposhnikov, A. V.,Fedoseev, V. M.
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p. 1777 - 1782
(2007/10/02)
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- EFFECT OF VICINAL SUBSTITUENTS ON REACTIVITY IN BIMOLECULAR NUCLEOPHILIC SUBSTITUTION AT A SATURATED CARBON ATOM. TWO TYPES OF SUBSTITUENT I. KINETICS OF THE REACTIONS OF THIOUREA WITH β-SUBSTITUTED BROMOETHANES IN DIMETHYLFORMAMIDE
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The kinetics of the reaction of thiourea with β-substituted bromoethanes in DMFA were studied by radiochromatography.It was shown that there is no isokinetic relationship or Taft equation for all the substituents but that there are isokinetic relationships for two separate reaction series, one of which is described satisfactorily by a Taft equation taking account of the inductive and steric effects of the substituents.On the basis of the obtained data it is supposed that there are two types of vicinal substituents, which affect the reactivity of the bromine at the saturated carbon atom by different mechanisms.For the first type of substituent (H, F, Br, CH3, C6H5) the main factors determining the reactivity are the inductive and steric effects of the substituents.Substituents of the second type (COOH, COOC2H5, CN, NH3Br, SC(NH2)2Br) include charged or highly polar substituents, and this makes it possible to expect a field effect, leading to additional stabilization of the transition state.
- Ryazantsev, G. B.,Lys, Ya. I.,Fedoseev, V. M.
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p. 776 - 779
(2007/10/02)
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- SYNTHESIS OF MONO(ALKYLTHIO)-SUBSTITUTED KETONES
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In the reaction of 2-propanone in the presence of sodium bicarbonate with a mixture of formaldehyde and the corresponding alkaline hydrolyzates of S-alkylthiuronium salts (thioalcoholates) β-keto sulfides (1-alkylthio-3-butanones) were obtained.Ketalization of the products with glycerol gave the cyclic derivatives alkylthio-1,3-dioxolanes.
- Sabirov, S. S.,Gnevasheva, L. M.,Ismailov, M. I.,Isobaev, M. D.
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p. 1239 - 1243
(2007/10/02)
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