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Les liquides ioniques dans la réaction d’hétéro-cyclisation intramoléculaire de 2-aminochalcones et 2-époxychalcones / Meryem Chelghoum
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Titre : Les liquides ioniques dans la réaction d’hétéro-cyclisation intramoléculaire de 2-aminochalcones et 2-époxychalcones : Synthése et évaluation biologique de dérivés de l’imidazole quaternairisés hautement fonctionnalisés. Type de document : texte imprimé Auteurs : Meryem Chelghoum, Auteur ; Ali Belfaitah, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2018 Importance : 165 f. Format : 30 cm. Note générale : Doctorat 3éme CYCLE LMD.
2 copies imprimées disponibles
Langues : Français (fre) Catégories : Français - Anglais
ChimieTags : Chimie: chimie organique Liquides ioniques Aza-analogues de flavonoïdes Cyclisation intramoléculaire Imidazole O834 Fonctionnalisation Sels d’imidazolium Activité biologique ionic liquid intramolecular hetero-cyclization imidazolium salt antibacterial activity سوائل أيونية مشابهات الفلافونويدات تفاعل حرلقي داخل الجزيء ايميدازول املاح ايميدازول نشاط البيولوجي Index. décimale : 540 Chimie et sciences connexes Résumé :
Two distinct themes were discussed during this thesis. The first concerns the synthesis and the use of ionic liquids in the intramolecular hetero-cyclization reaction of 2-aminochalcones and 1,2-epoxy-2-aminochalcones, while the second relates to the preparation and evaluation of antibacterial activity of quaternized poly-functionalized imidazolium salts. In the first part dedicated (reserved) to the isomerization reaction of 2-aminochalcones and 2- aminochalcones epoxides in ionic liquid environment, we have shown that the reaction proceeds correctly, and it is applicable to a wide range of substrates, without the use of an additional catalyst. the cyclization of The derivatives of (E) -1- (2-aminophenyl) -3-phenylpropen-2- en-1-one were tested in Three ionic liquids [bPy] [BF4], [bmim] [BF4] and [bmim] [PF6], among these [bmim] [BF4] is the most efficient (ratio LI / substrate: 10/1, temperature: 150 ° C, reaction time: 2.5 h). The 2-aryl-2,3-dihydroquinolin-4 (1H) -ones have been obtained with satisfactory yields (70-92%) in ionic liquid [bmim] [BF4], the (this) latter is recyclable three times with a slight decrease in its catalytic activity (83 → 64%). We also reported a practical and effective protocol for the synthesis of 2-aryl-3-hydroxy-1,2,3,4- tetrahydroquinolin-4 (1H) -ones by an intramolecular cyclization reaction of epoxyde 2- aminochalcone in ionic liquid at 120 ° C (LI ratio / substrate: 5/1, temperature: 120 ° C, reaction time: 6 h) of the four ionic liquids investigated, [bmim] [OTf] gave the best results in terms of cyclized product yield (35-93%). The structures of the compounds prepared were elucidated by the usual spectroscopic methods (IR, 1H NMR and C-13), and other elemental analysis and Xray diffraction for some of them. In the second part, a whole series of highly functionalized imidazolium salt derivatives were prepared (12 compounds) and their structures elucidated by the usual spectroscopic methods (IR, 1H NMR and C-13) and by X-ray diffraction for some of them. Most of these compounds were evaluated for their inhibitory capacity against four pathogenic strains: three Gramnegative (Escherichia coli, Salmonella thipymurium and Pseudomonas aeruginosa) and one Gram-positive (Staphylococcus aureus) using two methods: the inhibition zone and the determination of the minimum inhibitory concentration (MIC). The MIC results shows that iodine derivatives have inhibitory activity against Gram-negative strains, superior to brominated derivatives and compounds bearing a nitro group. Staphylococcus aureus (Grampositive bacteria) are significantly less sensitive to the action of the substrates used.
Note de contenu :
Annexes.Diplôme : Doctorat En ligne : ../theses/chimie/CHE7406.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=11058 Les liquides ioniques dans la réaction d’hétéro-cyclisation intramoléculaire de 2-aminochalcones et 2-époxychalcones : Synthése et évaluation biologique de dérivés de l’imidazole quaternairisés hautement fonctionnalisés. [texte imprimé] / Meryem Chelghoum, Auteur ; Ali Belfaitah, Directeur de thèse . - جامعة الإخوة منتوري قسنطينة, 2018 . - 165 f. ; 30 cm.
Doctorat 3éme CYCLE LMD.
2 copies imprimées disponibles
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : Chimie: chimie organique Liquides ioniques Aza-analogues de flavonoïdes Cyclisation intramoléculaire Imidazole O834 Fonctionnalisation Sels d’imidazolium Activité biologique ionic liquid intramolecular hetero-cyclization imidazolium salt antibacterial activity سوائل أيونية مشابهات الفلافونويدات تفاعل حرلقي داخل الجزيء ايميدازول املاح ايميدازول نشاط البيولوجي Index. décimale : 540 Chimie et sciences connexes Résumé :
Two distinct themes were discussed during this thesis. The first concerns the synthesis and the use of ionic liquids in the intramolecular hetero-cyclization reaction of 2-aminochalcones and 1,2-epoxy-2-aminochalcones, while the second relates to the preparation and evaluation of antibacterial activity of quaternized poly-functionalized imidazolium salts. In the first part dedicated (reserved) to the isomerization reaction of 2-aminochalcones and 2- aminochalcones epoxides in ionic liquid environment, we have shown that the reaction proceeds correctly, and it is applicable to a wide range of substrates, without the use of an additional catalyst. the cyclization of The derivatives of (E) -1- (2-aminophenyl) -3-phenylpropen-2- en-1-one were tested in Three ionic liquids [bPy] [BF4], [bmim] [BF4] and [bmim] [PF6], among these [bmim] [BF4] is the most efficient (ratio LI / substrate: 10/1, temperature: 150 ° C, reaction time: 2.5 h). The 2-aryl-2,3-dihydroquinolin-4 (1H) -ones have been obtained with satisfactory yields (70-92%) in ionic liquid [bmim] [BF4], the (this) latter is recyclable three times with a slight decrease in its catalytic activity (83 → 64%). We also reported a practical and effective protocol for the synthesis of 2-aryl-3-hydroxy-1,2,3,4- tetrahydroquinolin-4 (1H) -ones by an intramolecular cyclization reaction of epoxyde 2- aminochalcone in ionic liquid at 120 ° C (LI ratio / substrate: 5/1, temperature: 120 ° C, reaction time: 6 h) of the four ionic liquids investigated, [bmim] [OTf] gave the best results in terms of cyclized product yield (35-93%). The structures of the compounds prepared were elucidated by the usual spectroscopic methods (IR, 1H NMR and C-13), and other elemental analysis and Xray diffraction for some of them. In the second part, a whole series of highly functionalized imidazolium salt derivatives were prepared (12 compounds) and their structures elucidated by the usual spectroscopic methods (IR, 1H NMR and C-13) and by X-ray diffraction for some of them. Most of these compounds were evaluated for their inhibitory capacity against four pathogenic strains: three Gramnegative (Escherichia coli, Salmonella thipymurium and Pseudomonas aeruginosa) and one Gram-positive (Staphylococcus aureus) using two methods: the inhibition zone and the determination of the minimum inhibitory concentration (MIC). The MIC results shows that iodine derivatives have inhibitory activity against Gram-negative strains, superior to brominated derivatives and compounds bearing a nitro group. Staphylococcus aureus (Grampositive bacteria) are significantly less sensitive to the action of the substrates used.
Note de contenu :
Annexes.Diplôme : Doctorat En ligne : ../theses/chimie/CHE7406.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=11058 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité CHE/7406 CHE/7406 Thèse Bibliothèque principale Thèses Disponible Conception et evaluation de l’activité biologique de nouveaux dérivés indoliziniques et furaniques et expérimentation de nouveaux procédés pour l’obtention de flavonols. / Roumaissa Belguedj
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Titre : Conception et evaluation de l’activité biologique de nouveaux dérivés indoliziniques et furaniques et expérimentation de nouveaux procédés pour l’obtention de flavonols. Type de document : texte imprimé Auteurs : Roumaissa Belguedj, Auteur ; Abdelmalek Bouraiou, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2018 Importance : 247 f. Format : 30 cm. Note générale : Doctorat 3éme CYCLE LMD.
2 copies imprimées disponibles
Langues : Français (fre) Catégories : Français - Anglais
ChimieTags : Chimie: chimie organique ylure de pyridinium cycloaddition 1,3-dipolaire réactions multicomposants micro-ondes indolizine 2,3-dihydrofurane flavonoïdes réaction AFO mécanochimie liquides ioniques activités biologiques pyridinium ylide 1,3-dipolar cycloaddition multi-component reactions microwaves 2,3-dihydrofuran flavonoids AFO reaction Mechanochemistry ionic liquids Biological activity إلير البيريدينيوم تفاعل اN1ضافة الحلقية- 3,1ثنائي القطب تفاعل متعدد المكونات ميكروايف، الف67فونويد, تفاعل ) AFOال( كيمياء لا ميكانيكية ال سوائل أيونية النشاط البيولوجي Index. décimale : 540 Chimie et sciences connexes Résumé :
The aim of the first part of this work is the elaboration of new hybrid compounds containing different heterocycles such as indolizine, benzindolizine, imidazole, quinoline, benzimidazole or furan by the exploitation of the reactivity of some pyridinium-based ylides having the imidazole, benzimidazole or quinoline nucleus. The prepared compounds were subjected to biological evaluation. This part is subdivided into 3 chapters: In the first chapter, the biological activities and some synthesis methods of indolizine derivatives as well as some concepts about the 1,3-dipolar cycloaddition reaction were given. The results concerning the synthesis of the hybrid derivatives (benz) indolizine / (benz) imidazole and indolizine / quinoline were presented in an experimental part. In the second chapter, after a brief bibliographical overview concerning biological applications of some 2,3-dihydrofuran derivatives, we have presented the most widely used synthetic methods for this class of compounds. The discussion of the results concerning the synthesis of the benzimidazole / 2,3-dihydrofuran hybrid derivatives via the multicomponent reaction were discussed in the next section. In the third chapter, which was devoted to the biological evaluation of certain prepared compounds, some basic notions about this part (tuberculosis, leishmaniasis and oxidative stress) were given. The results that we have obtained, were exposed and commented in results and discussion part. The second part of this work is in relation with modern chemistry. This part was devoted to the experimentation of the AFO reaction by two modern approaches (mechanochemistry and the use of ionic liquids). After a bibliographic overview of some modern synthesis technologies and alternatives methodes to volatile solvents, the results obtained were discussed in the results and discussion section. Each part was closed by an experimental section which details the experimental protocols, as well as the spectroscopic and physical characteristics of the compounds obtained. The molecules prepared have been identified by the usual spectral methods such as IR, 1H and 13C NMR. The original products have been further characterized by high resolution mass spectroscopy and / or X-ray diffraction.
Note de contenu :
Annexes.Diplôme : Doctorat En ligne : ../theses/chimie/BEL7407.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=11059 Conception et evaluation de l’activité biologique de nouveaux dérivés indoliziniques et furaniques et expérimentation de nouveaux procédés pour l’obtention de flavonols. [texte imprimé] / Roumaissa Belguedj, Auteur ; Abdelmalek Bouraiou, Directeur de thèse . - جامعة الإخوة منتوري قسنطينة, 2018 . - 247 f. ; 30 cm.
Doctorat 3éme CYCLE LMD.
2 copies imprimées disponibles
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : Chimie: chimie organique ylure de pyridinium cycloaddition 1,3-dipolaire réactions multicomposants micro-ondes indolizine 2,3-dihydrofurane flavonoïdes réaction AFO mécanochimie liquides ioniques activités biologiques pyridinium ylide 1,3-dipolar cycloaddition multi-component reactions microwaves 2,3-dihydrofuran flavonoids AFO reaction Mechanochemistry ionic liquids Biological activity إلير البيريدينيوم تفاعل اN1ضافة الحلقية- 3,1ثنائي القطب تفاعل متعدد المكونات ميكروايف، الف67فونويد, تفاعل ) AFOال( كيمياء لا ميكانيكية ال سوائل أيونية النشاط البيولوجي Index. décimale : 540 Chimie et sciences connexes Résumé :
The aim of the first part of this work is the elaboration of new hybrid compounds containing different heterocycles such as indolizine, benzindolizine, imidazole, quinoline, benzimidazole or furan by the exploitation of the reactivity of some pyridinium-based ylides having the imidazole, benzimidazole or quinoline nucleus. The prepared compounds were subjected to biological evaluation. This part is subdivided into 3 chapters: In the first chapter, the biological activities and some synthesis methods of indolizine derivatives as well as some concepts about the 1,3-dipolar cycloaddition reaction were given. The results concerning the synthesis of the hybrid derivatives (benz) indolizine / (benz) imidazole and indolizine / quinoline were presented in an experimental part. In the second chapter, after a brief bibliographical overview concerning biological applications of some 2,3-dihydrofuran derivatives, we have presented the most widely used synthetic methods for this class of compounds. The discussion of the results concerning the synthesis of the benzimidazole / 2,3-dihydrofuran hybrid derivatives via the multicomponent reaction were discussed in the next section. In the third chapter, which was devoted to the biological evaluation of certain prepared compounds, some basic notions about this part (tuberculosis, leishmaniasis and oxidative stress) were given. The results that we have obtained, were exposed and commented in results and discussion part. The second part of this work is in relation with modern chemistry. This part was devoted to the experimentation of the AFO reaction by two modern approaches (mechanochemistry and the use of ionic liquids). After a bibliographic overview of some modern synthesis technologies and alternatives methodes to volatile solvents, the results obtained were discussed in the results and discussion section. Each part was closed by an experimental section which details the experimental protocols, as well as the spectroscopic and physical characteristics of the compounds obtained. The molecules prepared have been identified by the usual spectral methods such as IR, 1H and 13C NMR. The original products have been further characterized by high resolution mass spectroscopy and / or X-ray diffraction.
Note de contenu :
Annexes.Diplôme : Doctorat En ligne : ../theses/chimie/BEL7407.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=11059 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité BEL/7407 BEL/7407 Thèse Bibliothèque principale Thèses Disponible Élaboration de nouvelles voies catalytiques dans la synthese de molécules hétérocycliques / Faiza Boukezzoula
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Titre : Élaboration de nouvelles voies catalytiques dans la synthese de molécules hétérocycliques Type de document : texte imprimé Auteurs : Faiza Boukezzoula, Auteur ; Taoues Boumoud, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2016 Importance : 196 f. Format : 30 cm. Note générale : 2 copies imprimées disponibles
Langues : Français (fre) Catégories : Français - Anglais
ChimieTags : hétérocycles synthèse convergente réactions à composants multiples catalyse
organique molécules chirales et achirales synthèse asymétrique liquides ioniques pyrazolopyranopyrimidines pyranopyrazoles spirooxindoles heterocyclic compounds convergent strategy MCRs Organocatalysis asymmetrical and symmetrical molecules asymmetric synthesis ionic liquids المركبات الحلقية الغير متجانسة التفاعلات الكيماوية المتعددة المتفاعلات المحفزات العضوية المركبات الكيرالية ولاكيرالية السوائل الأيونية بيرازولوبيرانوابيرميدين بيرنوابيرازول سبيروا اكسندولIndex. décimale : 540 Chimie et sciences connexes Résumé : The subject that we developed "Elaboration of novel catalytic methods for the synthesis of
heterocyclic molecules " summarizes:
- Through a bibliographical study which puts forward the heterocyclic compounds, the advantage of the reactions making their synthesis possible, in occurrence MCRs and the privilege of organic catalysis.
- Through a study of the catalytic properties of two molecules asymmetrical (DMAP and DABCO) and two symmetrical (L-Proline and Cinchonine) with respect to the synthesis of
pyrazolpyrnopyrimidindiones/ones and pyranopyrazoles, via multicomponent reactions
- Through a study of catalytic properties of two ionic liquids [MePPh3][Br] and [OPPh3][Br] in the synthesis of the spirooxindoles and the pyranopyrazoles. The results with [OPPh3][Br] are not as good as those obtained with [MePPh3][Br], which certainly due to its cumbersome properties.
- This study reinforced the idea of the organic catalysis in MCRs giving the
pyrazolopyranopyrimidindiones/ones the pyranopyrazoles and the spirooxindoles
heterocyclic compoundsDiplôme : Doctorat En ligne : ../theses/chimie/BOU6898.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=10228 Élaboration de nouvelles voies catalytiques dans la synthese de molécules hétérocycliques [texte imprimé] / Faiza Boukezzoula, Auteur ; Taoues Boumoud, Directeur de thèse . - جامعة الإخوة منتوري قسنطينة, 2016 . - 196 f. ; 30 cm.
2 copies imprimées disponibles
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : hétérocycles synthèse convergente réactions à composants multiples catalyse
organique molécules chirales et achirales synthèse asymétrique liquides ioniques pyrazolopyranopyrimidines pyranopyrazoles spirooxindoles heterocyclic compounds convergent strategy MCRs Organocatalysis asymmetrical and symmetrical molecules asymmetric synthesis ionic liquids المركبات الحلقية الغير متجانسة التفاعلات الكيماوية المتعددة المتفاعلات المحفزات العضوية المركبات الكيرالية ولاكيرالية السوائل الأيونية بيرازولوبيرانوابيرميدين بيرنوابيرازول سبيروا اكسندولIndex. décimale : 540 Chimie et sciences connexes Résumé : The subject that we developed "Elaboration of novel catalytic methods for the synthesis of
heterocyclic molecules " summarizes:
- Through a bibliographical study which puts forward the heterocyclic compounds, the advantage of the reactions making their synthesis possible, in occurrence MCRs and the privilege of organic catalysis.
- Through a study of the catalytic properties of two molecules asymmetrical (DMAP and DABCO) and two symmetrical (L-Proline and Cinchonine) with respect to the synthesis of
pyrazolpyrnopyrimidindiones/ones and pyranopyrazoles, via multicomponent reactions
- Through a study of catalytic properties of two ionic liquids [MePPh3][Br] and [OPPh3][Br] in the synthesis of the spirooxindoles and the pyranopyrazoles. The results with [OPPh3][Br] are not as good as those obtained with [MePPh3][Br], which certainly due to its cumbersome properties.
- This study reinforced the idea of the organic catalysis in MCRs giving the
pyrazolopyranopyrimidindiones/ones the pyranopyrazoles and the spirooxindoles
heterocyclic compoundsDiplôme : Doctorat En ligne : ../theses/chimie/BOU6898.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=10228 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité BOU/6898 BOU/6898 Thèse Bibliothèque principale Thèses Disponible
Titre : Synthèse et caractérisation de poly-hétérocycles bioactifs Type de document : texte imprimé Auteurs : Chamseddine Derabli, Auteur ; Raouf Boulcina, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2016 Importance : 217 f. Format : 30 cm. Note générale : 2 copies imprimées disponibles
Langues : Français (fre) Catégories : Français - Anglais
ChimieTags : Quinolones cyclisation d’aza-Michael liquides ioniques quinazolines quinazolinones quinoléines pyranopyrazoles pyrimidines Tacrine Maladie d’Alzheimer aza-Michael cyclization ionic liquids quinolines Alzheimer's disease الكينولونات تحلق آزا-ميكائيل السائل الأيوني كينازولينات كينازولينونات كينولين بيرانوبيرازول بيريميدين تاكرين مرض
الألزهايمرIndex. décimale : 540 Chimie et sciences connexes Résumé : This manuscript includes three main parts:
In the first chapter, we described a new method for preparation of 2-aryl-2,3-dihydro-4-quinolonesby the use of the cyclization of the corresponding 2-aminochalconesvia an azaMichael reaction. This method was catalyzed by a DABCO’s ionic liquid which allowed us to obtain quantitatively our intended products in a single step.
In the second chapter, we synthesized a series of new 1,2-dihydroquinazoline derivatives by a one pot reaction, from benzaldehyde derivatives, ammonium acetate and 2-aminobenzophenones in the presence of DMAP. Similarly, we described the synthesis of new hybrid quinazoline-quinoline compounds from raw materials and other easily accessible key intermediates.
Finally, the study that we have undertaken in this final chapter of the thesis has as main objective, the preparation of novel heterocyclic analogues of Tacrine (used in the treatment of Alzheimer's disease) based pyranopyrazole and pyrimidine structures.
Diplôme : Doctorat Permalink : index.php?lvl=notice_display&id=10221 Synthèse et caractérisation de poly-hétérocycles bioactifs [texte imprimé] / Chamseddine Derabli, Auteur ; Raouf Boulcina, Directeur de thèse . - جامعة الإخوة منتوري قسنطينة, 2016 . - 217 f. ; 30 cm.
2 copies imprimées disponibles
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : Quinolones cyclisation d’aza-Michael liquides ioniques quinazolines quinazolinones quinoléines pyranopyrazoles pyrimidines Tacrine Maladie d’Alzheimer aza-Michael cyclization ionic liquids quinolines Alzheimer's disease الكينولونات تحلق آزا-ميكائيل السائل الأيوني كينازولينات كينازولينونات كينولين بيرانوبيرازول بيريميدين تاكرين مرض
الألزهايمرIndex. décimale : 540 Chimie et sciences connexes Résumé : This manuscript includes three main parts:
In the first chapter, we described a new method for preparation of 2-aryl-2,3-dihydro-4-quinolonesby the use of the cyclization of the corresponding 2-aminochalconesvia an azaMichael reaction. This method was catalyzed by a DABCO’s ionic liquid which allowed us to obtain quantitatively our intended products in a single step.
In the second chapter, we synthesized a series of new 1,2-dihydroquinazoline derivatives by a one pot reaction, from benzaldehyde derivatives, ammonium acetate and 2-aminobenzophenones in the presence of DMAP. Similarly, we described the synthesis of new hybrid quinazoline-quinoline compounds from raw materials and other easily accessible key intermediates.
Finally, the study that we have undertaken in this final chapter of the thesis has as main objective, the preparation of novel heterocyclic analogues of Tacrine (used in the treatment of Alzheimer's disease) based pyranopyrazole and pyrimidine structures.
Diplôme : Doctorat Permalink : index.php?lvl=notice_display&id=10221 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité DER/6892 DER/6892 Thèse Bibliothèque principale Thèses Disponible