Pub Date : 2015-01-30DOI: 10.2174/1874095201509010001
E. Macleod, K. Vaughan
New triazenes derived from the 1-alkylpiperazines have been synthesized. Each 1-alkylpiperazine was treated with a diazonium salt solution to produce the new triazenes, which have been characterized by proton and carbon- 13 NMR spectroscopy, IR spectroscopy and by mass spectrometric analysis. Assignment of the chemical shifts to specific protons and carbons in the piperazine ring was facilitated by comparison with the chemical shifts in the previously reported 1-methyl-4-(2-aryl-1-diazenyl)piperazines (1).
{"title":"Synthesis and Characterization of New Compounds in the Series 1-alkyl-4- (2-aryl-1-diazenyl)piperazines","authors":"E. Macleod, K. Vaughan","doi":"10.2174/1874095201509010001","DOIUrl":"https://doi.org/10.2174/1874095201509010001","url":null,"abstract":"New triazenes derived from the 1-alkylpiperazines have been synthesized. Each 1-alkylpiperazine was treated with a diazonium salt solution to produce the new triazenes, which have been characterized by proton and carbon- 13 NMR spectroscopy, IR spectroscopy and by mass spectrometric analysis. Assignment of the chemical shifts to specific protons and carbons in the piperazine ring was facilitated by comparison with the chemical shifts in the previously reported 1-methyl-4-(2-aryl-1-diazenyl)piperazines (1).","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"1 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2015-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75936092","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2015-01-30DOI: 10.2174/1874095201509010009
L. Troisi, C. Citti, C. Granito, S. Perrone, A. Ciccarese, S. Bettini, G. Giancane, A. Troisi
New perylene monoimides, diimides and bis-diimides have been designed and synthetized. A detailed investigation of the synthesis of these compounds has also been performed in order to highlight the crucial factors for obtaining a specific class of molecules. Specifically, the attention has been focused on the synthesis of the intermediate perylene monoimides which are very useful precursors for many molecules difficult to obtain. Furthemore, two synthetic pathways have been developed for obtaining the bis-diimides variously substituted. These final compounds are predicted to mimic the excellent electron acceptor properties of fullerene derivatives and they can be used as building blocks to form 3D semiconducting materials.
{"title":"Synthesis of Alternative Electron Acceptor Compounds","authors":"L. Troisi, C. Citti, C. Granito, S. Perrone, A. Ciccarese, S. Bettini, G. Giancane, A. Troisi","doi":"10.2174/1874095201509010009","DOIUrl":"https://doi.org/10.2174/1874095201509010009","url":null,"abstract":"New perylene monoimides, diimides and bis-diimides have been designed and synthetized. A detailed investigation of the synthesis of these compounds has also been performed in order to highlight the crucial factors for obtaining a specific class of molecules. Specifically, the attention has been focused on the synthesis of the intermediate perylene monoimides which are very useful precursors for many molecules difficult to obtain. Furthemore, two synthetic pathways have been developed for obtaining the bis-diimides variously substituted. These final compounds are predicted to mimic the excellent electron acceptor properties of fullerene derivatives and they can be used as building blocks to form 3D semiconducting materials.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"118 1","pages":"9-15"},"PeriodicalIF":0.0,"publicationDate":"2015-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75361962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2014-11-14DOI: 10.2174/1874095201408010019
S. Höppner, N. Schlörer, W. Schänzer, M. Thevis
The enzyme sirtuin 1 (SIRT1) is a major target for the treatment of various metabolic disorders. Herein, a practical synthesis of imidazo(1,2-b)thiazole derivatives, one of the most comprehensively studied class of synthetic SIRT1 activators, is presented. The synthesized SIRT1 activators, the in vitro-identified metabolite of SRT1720, and the eightfold deuterated analytical standards were obtained through a six-step protocol yielding model compounds with a conserved core structure and two variable moieties. A multiplicity of potential SIRT1 activators and metabolites can be prepared with substituents enabling the modification of biological effects.
{"title":"Synthesis of Four SIRT1 Activators Based on an Imidazo(1,2-b)thiazole Structure, in vitro Derived Metabolites and Deuterated Analogs","authors":"S. Höppner, N. Schlörer, W. Schänzer, M. Thevis","doi":"10.2174/1874095201408010019","DOIUrl":"https://doi.org/10.2174/1874095201408010019","url":null,"abstract":"The enzyme sirtuin 1 (SIRT1) is a major target for the treatment of various metabolic disorders. Herein, a practical synthesis of imidazo(1,2-b)thiazole derivatives, one of the most comprehensively studied class of synthetic SIRT1 activators, is presented. The synthesized SIRT1 activators, the in vitro-identified metabolite of SRT1720, and the eightfold deuterated analytical standards were obtained through a six-step protocol yielding model compounds with a conserved core structure and two variable moieties. A multiplicity of potential SIRT1 activators and metabolites can be prepared with substituents enabling the modification of biological effects.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"6 1","pages":"19-23"},"PeriodicalIF":0.0,"publicationDate":"2014-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78949106","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2014-10-28DOI: 10.2174/1874095201408010015
Durga Pokharel, Shiyue Fang
Purification of synthetic oligodeoxynucleotides (ODNs) is simply achieved by capping failure sequences with a polymerizable phosphoramidite followed by polymerization. In this article, the reduction of the amount of polymerization monomer to drastically increase ODN extraction efficiency, the use of a centrifugal filterunit to ease the extraction process and the notification of using fresh phosphoramidite solutions are described. In addition, further evidence to support the purity of ODN and discussions of ODN stability under radical polymerization conditions are provided.
{"title":"A Highly Convenient Procedure for Oligodeoxynucleotide Purification","authors":"Durga Pokharel, Shiyue Fang","doi":"10.2174/1874095201408010015","DOIUrl":"https://doi.org/10.2174/1874095201408010015","url":null,"abstract":"Purification of synthetic oligodeoxynucleotides (ODNs) is simply achieved by capping failure sequences with a polymerizable phosphoramidite followed by polymerization. In this article, the reduction of the amount of polymerization monomer to drastically increase ODN extraction efficiency, the use of a centrifugal filterunit to ease the extraction process and the notification of using fresh phosphoramidite solutions are described. In addition, further evidence to support the purity of ODN and discussions of ODN stability under radical polymerization conditions are provided.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"35 1","pages":"15-18"},"PeriodicalIF":0.0,"publicationDate":"2014-10-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86518537","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2014-05-30DOI: 10.2174/1874095201408010001
M. Forouzani, H. Ghasemnejad-Bosra
New and convenient one-pot syntheses of 2-substituted aryl (indolyl) kojyl thioether from 2-substituted aryl (indolyl) kojic acids have been found. Firstly, the 2-substituted aryl (indolyl) kojic acids were readily obtained from cou- pling of aldehyde, kojic acid and indoles in the presence of p-toluenesulfonic acid as catalyst in good yields and with high selectivity. Then, 2-substituted aryl (indolyl) kojic acids were reacted with thionyl chloride to afford corresponding 2- substituted aryl (indolyl) kojic chlorides. Finally, the 2-substituted aryl (indolyl) kojic chloride derivatives were reacted with benzenethiols in presence of triethylamine in t etrahydrofurane to afford the corresponding thioether derivatives in good yields.
{"title":"Efficient One-pot pTSA-catalyzed Synthesis of 2-substituted Aryl (indolyl)kojic Acid and Kojyl Thioether Derivatives Under Mild Conditions","authors":"M. Forouzani, H. Ghasemnejad-Bosra","doi":"10.2174/1874095201408010001","DOIUrl":"https://doi.org/10.2174/1874095201408010001","url":null,"abstract":"New and convenient one-pot syntheses of 2-substituted aryl (indolyl) kojyl thioether from 2-substituted aryl (indolyl) kojic acids have been found. Firstly, the 2-substituted aryl (indolyl) kojic acids were readily obtained from cou- pling of aldehyde, kojic acid and indoles in the presence of p-toluenesulfonic acid as catalyst in good yields and with high selectivity. Then, 2-substituted aryl (indolyl) kojic acids were reacted with thionyl chloride to afford corresponding 2- substituted aryl (indolyl) kojic chlorides. Finally, the 2-substituted aryl (indolyl) kojic chloride derivatives were reacted with benzenethiols in presence of triethylamine in t etrahydrofurane to afford the corresponding thioether derivatives in good yields.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"21 1","pages":"1-5"},"PeriodicalIF":0.0,"publicationDate":"2014-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85192638","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-11-29DOI: 10.2174/1874095201307010015
Yanmei Zhang, Weixing Dan, Jianqi Liu, M. Tortorella, Zheng-chao Tu, J. Talley
Palladium catalysis is an efficient way to obtain trimethylsilyl substituted benzopyran derivatives. After screen- ing a series of reactions , we found optimized conditions.
钯催化是制备三甲基硅基取代苯并吡喃衍生物的有效途径。通过对一系列反应的筛选，找到了最佳的反应条件。
{"title":"Palladium-Catalyzed Synthesis of Trimethylsilyl Substituted Benzopyran Derivatives","authors":"Yanmei Zhang, Weixing Dan, Jianqi Liu, M. Tortorella, Zheng-chao Tu, J. Talley","doi":"10.2174/1874095201307010015","DOIUrl":"https://doi.org/10.2174/1874095201307010015","url":null,"abstract":"Palladium catalysis is an efficient way to obtain trimethylsilyl substituted benzopyran derivatives. After screen- ing a series of reactions , we found optimized conditions.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"135 1","pages":"15-20"},"PeriodicalIF":0.0,"publicationDate":"2013-11-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80049256","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-07-12DOI: 10.2174/1874095220130529001
B. Rasmussen, J. B. Christensen
A series of mono protected ,-diamines protected with photolabile carbamates has been synthesized by reac- tion between the corresponding ,-diamines and either o-nitrobenzyl or 1-(2-nitrophenyl)ethyl phenyl carbonate.
{"title":"Facile Synthesis of o-Nitrobenzylcarbamate and 1-(2-Nitrophenyl ethyl) Carbamate Protected α,-Diamines","authors":"B. Rasmussen, J. B. Christensen","doi":"10.2174/1874095220130529001","DOIUrl":"https://doi.org/10.2174/1874095220130529001","url":null,"abstract":"A series of mono protected ,-diamines protected with photolabile carbamates has been synthesized by reac- tion between the corresponding ,-diamines and either o-nitrobenzyl or 1-(2-nitrophenyl)ethyl phenyl carbonate.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"7 1","pages":"11-14"},"PeriodicalIF":0.0,"publicationDate":"2013-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79541601","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-04-30DOI: 10.2174/1874095201307010001
O. Ajani, O. Familoni, J. O. Echeme, Feipeng Wu
An highly expeditious synthetic approach for the synthesis of benzenemethanesulfonamides (1a-k) and their new corresponding N,N-diethyl substituted amido moieties (2a-k) has been achieved in aqueous medium at room tem- perature. The reaction condition was thoroughly optimized thereby allowing significant rate enhancement and resulting into excellent yields. The chemical structures of the successful candidates were confirmed using elemental analytical and spectroscopic data such as IR, 1 H NMR, 13 C NMR and some selected mass spectral data. Graphical Abstract Environmental friendly synthesis of new N,N-diethyl-substituted-2-(phenylmethylsulfo namido)alkanamide derivatives was achieved in aqueous medium via synthetic modification of the benzenemethanesulfonamide precursors.
{"title":"Ecofriendly Synthesis in Aqueous Medium: An Expeditious Approach to New N,N-Diethyl Amide Bearing Benzenemethanesulfonamides","authors":"O. Ajani, O. Familoni, J. O. Echeme, Feipeng Wu","doi":"10.2174/1874095201307010001","DOIUrl":"https://doi.org/10.2174/1874095201307010001","url":null,"abstract":"An highly expeditious synthetic approach for the synthesis of benzenemethanesulfonamides (1a-k) and their new corresponding N,N-diethyl substituted amido moieties (2a-k) has been achieved in aqueous medium at room tem- perature. The reaction condition was thoroughly optimized thereby allowing significant rate enhancement and resulting into excellent yields. The chemical structures of the successful candidates were confirmed using elemental analytical and spectroscopic data such as IR, 1 H NMR, 13 C NMR and some selected mass spectral data. Graphical Abstract Environmental friendly synthesis of new N,N-diethyl-substituted-2-(phenylmethylsulfo namido)alkanamide derivatives was achieved in aqueous medium via synthetic modification of the benzenemethanesulfonamide precursors.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"61 1","pages":"1-10"},"PeriodicalIF":0.0,"publicationDate":"2013-04-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91291828","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2012-06-22DOI: 10.2174/1874095201206010021
A. Fall, O. Diouf, M. Gaye, Generosa Gómez
We describe the preparation and use of two new imidazolium-bound Rose Bengal derivatives for singlet oxy- gen generation. Photolysis of oxygen-saturated solution of furan rings in the presence of the imidazolium-bound sensitiz- ers provides the corresponding butenolides. The sensitizers could be recovered after the oxidation reaction.
{"title":"Synthesis and Use of Imidazolium Bound Rose Bengal Derivatives for Singlet Oxygen Generation","authors":"A. Fall, O. Diouf, M. Gaye, Generosa Gómez","doi":"10.2174/1874095201206010021","DOIUrl":"https://doi.org/10.2174/1874095201206010021","url":null,"abstract":"We describe the preparation and use of two new imidazolium-bound Rose Bengal derivatives for singlet oxy- gen generation. Photolysis of oxygen-saturated solution of furan rings in the presence of the imidazolium-bound sensitiz- ers provides the corresponding butenolides. The sensitizers could be recovered after the oxidation reaction.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"38 1","pages":"21-26"},"PeriodicalIF":0.0,"publicationDate":"2012-06-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81479635","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2012-04-16DOI: 10.2174/1874095201206010012
A. Debache, Louisa Chouguiat, R. Boulcina, B. Carboni
The synthesis of various substituted Biginelli 3,4-dihydropyrimidinone/thione and Hantzsch 1,4- dihydropyridine derivatives has been achieved using a modified procedure in the presence of potassium ter-butoxide (t- BuOK) as a catalyst under solvent-free conditions, in good to excellent yields.
{"title":"A One-pot Multi-component Synthesis of Dihydropyrimidinone/Thione and Dihydropyridine Derivatives via Biginelli and Hantzsch Condensations using t-BuOK as a Catalyst Under Solvent-free Conditions","authors":"A. Debache, Louisa Chouguiat, R. Boulcina, B. Carboni","doi":"10.2174/1874095201206010012","DOIUrl":"https://doi.org/10.2174/1874095201206010012","url":null,"abstract":"The synthesis of various substituted Biginelli 3,4-dihydropyrimidinone/thione and Hantzsch 1,4- dihydropyridine derivatives has been achieved using a modified procedure in the presence of potassium ter-butoxide (t- BuOK) as a catalyst under solvent-free conditions, in good to excellent yields.","PeriodicalId":23020,"journal":{"name":"The Open Organic Chemistry Journal","volume":"89 1","pages":"12-20"},"PeriodicalIF":0.0,"publicationDate":"2012-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75908728","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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