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Synthesis and structural characterization of novel benzothiazole derivatives
No full textU ovom radu opisana je sinteza novih derivata benzotiazola primjenom mikrovalovima potpomognutih, mehanokemijskih i klik reakcija. Za sintezu derivata benzotiazola pripravljen je 4-O-propargilbenzaldehid (1) SN2 reakcijom 4-hidroksibenzaldehida i propargil-bromida uz K2CO3 kao bazu. 2-(4-(prop-2-in-1-iloksi)fenil)benzotiazol (2) priređen je ciklizacijom
4-O-propargilbenzaldehida (1) i 2-aminotiofenola u dimetilformamidu uz Na2S2O5 kao oksidacijsko sredstvo. Huisgenovom 1,3-dipolarnom cikloadicijom
2-(4-(prop-2-in-1-iloksi)fenil)benzotiazola (2) i odgovarajućih azida uz bakrov(II) acetat kao katalizator sintetizirani su 1,2,3-triazolni derivati benzotiazola (3-9). Mehanokemijske reakcije ciljanih derivata benzotiazola (3-9) provedene su u kugličnom mlinu. 1H i 13C-NMR spektroskopijom potvrđene su strukture svih novopripravljenih derivata benzotiazola.This paper describes the synthesis of new benzothiazole derivatives using microwaveassisted, mechanochemical and click reactions. For the synthesis of benzothiazole derivatives, 4-O-propargylated benzaldehyde (1) was prepared by SN2 reaction of 4-hydroxybenzaldehyde and propargyl bromide using K2CO3 as a base.
2-(4-(prop-2-yn-1-yloxy)phenyl) benzothiazole (2) was prepared by cyclization reaction of 4-O-propargyl benzaldehyde (1) and 2-aminothiophenol in dimethylformamide with Na2S2O5 as oxidizing agent. 1,2,3-triazolyl derivatives of benzothiazole (3-9) were prepared by Huisgen 1,3-dipolar cycloaddition of 2-4-(prop-2-yn-1-yloxy)phenyl benzothiazole (2) and the corresponding azides using copper(II) acetate as catalyst. Mechanochemical reactions of the desired compounds (3-9) were performed in a ball mill. The structures of all newly prepared benzothiazole derivatives were confirmed by 1H and 13C-NMR spectroscopy
Synthesis, structural characterization and antibacterial activity of novel 2-hydrazone derivatives of benzothiazole
No full textU ovom radu opisana je sinteza ciljanih derivata benzotiazola premoštenih hidrazonskom spojnicom (3-14) i 1,2,3-triazolnih derivata benzotiazola (17-26) kao potencijalno biološki aktivnih agenasa te je provedena njihova strukturna karakterizacija spektroskopijom NMR. 2-amino-6-metoksibenzo[d]tiazol (1) sintetiziran je reakcijom ciklizacije p-metoksianilina s kalijevim tiocijanatom i bromom u octenoj kiselini koji je potom reakcijom nukleofilne supstitucije s hidrazin hidratom u prisustvu etilen-glikola i klorovodične kiseline preveden u 2-hidrazinil-6-metoksibenzo[d]tiazol (2). Benzotiazolni derivati hidrazona (3-14) pripremljeni su mehanokemijskim reakcijama 2-hidrazinil-6-metoksibenzo[d]tiazola (2) i odgovarajućih aldehida. Mikrovalovima potpomognutom reakcijom O-alkiliranja 3-hidroksi-4-metoksibenzaldehida s propargil-bromidom i kalijevim karbonatom kao bazom sintetiziran je 4-metoksi-3-(prop-2-in-1-iloksi)benzaldehid (15). Reakcijom kondenzacije spoja 15 i 2-aminotiofenola uz natrijev metabisulfit kao oksidacijsko sredstvo u dimetilformamidu pripravljen je 2-(4-metoksi-3-(prop-2-in-1-iloksi)fenil)benzo[d]tiazol (16). 1,2,3-triazolni derivati benzotiazola (17-26) sintetizirani su mehanokemijskom Huisgenovom 1,3-dipolarnom cikloadicijom spoja 16 i odgovarajućih azida u metanolu uz bakrov(II) acetat kao katalizator. Strukturna karakterizacija priređenih spojeva provedena je spektroskopijom 1H i 13C-NMR. In silico analizom predviđeni su farmakološki učinci i moguće biološke mete pripravljenih spojeva.In this paper, the synthesis of targeted benzothiazole derivatives bridged with a hydrazone coupling (3-14) and 1,2,3-triazole benzothiazole derivatives (17-26) as potentially biologically active agents is described, and their structural characterization by NMR spectroscopy was carried out. 2-amino-6-methoxybenzo[d]thiazole (1) was synthesized by the cyclization reaction of pmethoxyaniline with potassium thiocyanate and bromine in acetic acid, which was then converted into 2-hydrazinyl-6-methoxybenzo[d]thiazole (2) by reaction of nucleophilic substitution with hydrazine hydrate in the presence of ethylene glycol and hydrochloric acid. Benzothiazole hydrazone derivatives (3-14) were prepared by mechanochemical reactions of 2-hydrazinyl-6-methoxybenzo[d]thiazole (2) and corresponding aldehydes. 4-methoxy-3-(prop-2-yn-1-yloxy)benzaldehyde (15) was synthesized by microwave-assisted reaction of O-alkylation of 3-hydroxy-4-methoxybenzaldehyde with propargyl bromide and potassium carbonate as a base. 2-(4-methoxy-3-(prop-2-yn-1-yloxy)phenyl)benzo[d]thiazole (16) was prepared by the condensation reaction of compound 15 and 2-aminothiophenol with sodium metabisulfite as an oxidizing agent in dimethylformamide. 1,2,3-triazole derivatives of benzothiazole (17-26) were synthesized by mechanochemical Huisgen 1,3-dipolar cycloaddition of compound 16 and the corresponding azides in methanol with copper(II) acetate as a catalyst. Structural characterization of the prepared compounds was performed by 1H and 13C-NMR spectroscopy. Pharmacological effects and possible biological targets of the prepared compounds were predicted by in silico analysis
Synthesis and structural characterization of novel benzothiazole derivatives
No full textU ovom radu opisana je sinteza novih derivata benzotiazola primjenom mikrovalovima potpomognutih, mehanokemijskih i klik reakcija. Za sintezu derivata benzotiazola pripravljen je 4-O-propargilbenzaldehid (1) SN2 reakcijom 4-hidroksibenzaldehida i propargil-bromida uz K2CO3 kao bazu. 2-(4-(prop-2-in-1-iloksi)fenil)benzotiazol (2) priređen je ciklizacijom
4-O-propargilbenzaldehida (1) i 2-aminotiofenola u dimetilformamidu uz Na2S2O5 kao oksidacijsko sredstvo. Huisgenovom 1,3-dipolarnom cikloadicijom
2-(4-(prop-2-in-1-iloksi)fenil)benzotiazola (2) i odgovarajućih azida uz bakrov(II) acetat kao katalizator sintetizirani su 1,2,3-triazolni derivati benzotiazola (3-9). Mehanokemijske reakcije ciljanih derivata benzotiazola (3-9) provedene su u kugličnom mlinu. 1H i 13C-NMR spektroskopijom potvrđene su strukture svih novopripravljenih derivata benzotiazola.This paper describes the synthesis of new benzothiazole derivatives using microwaveassisted, mechanochemical and click reactions. For the synthesis of benzothiazole derivatives, 4-O-propargylated benzaldehyde (1) was prepared by SN2 reaction of 4-hydroxybenzaldehyde and propargyl bromide using K2CO3 as a base.
2-(4-(prop-2-yn-1-yloxy)phenyl) benzothiazole (2) was prepared by cyclization reaction of 4-O-propargyl benzaldehyde (1) and 2-aminothiophenol in dimethylformamide with Na2S2O5 as oxidizing agent. 1,2,3-triazolyl derivatives of benzothiazole (3-9) were prepared by Huisgen 1,3-dipolar cycloaddition of 2-4-(prop-2-yn-1-yloxy)phenyl benzothiazole (2) and the corresponding azides using copper(II) acetate as catalyst. Mechanochemical reactions of the desired compounds (3-9) were performed in a ball mill. The structures of all newly prepared benzothiazole derivatives were confirmed by 1H and 13C-NMR spectroscopy
Synthesis, structural characterization and antibacterial activity of novel 2-hydrazone derivatives of benzothiazole
No full textU ovom radu opisana je sinteza ciljanih derivata benzotiazola premoštenih hidrazonskom spojnicom (3-14) i 1,2,3-triazolnih derivata benzotiazola (17-26) kao potencijalno biološki aktivnih agenasa te je provedena njihova strukturna karakterizacija spektroskopijom NMR. 2-amino-6-metoksibenzo[d]tiazol (1) sintetiziran je reakcijom ciklizacije p-metoksianilina s kalijevim tiocijanatom i bromom u octenoj kiselini koji je potom reakcijom nukleofilne supstitucije s hidrazin hidratom u prisustvu etilen-glikola i klorovodične kiseline preveden u 2-hidrazinil-6-metoksibenzo[d]tiazol (2). Benzotiazolni derivati hidrazona (3-14) pripremljeni su mehanokemijskim reakcijama 2-hidrazinil-6-metoksibenzo[d]tiazola (2) i odgovarajućih aldehida. Mikrovalovima potpomognutom reakcijom O-alkiliranja 3-hidroksi-4-metoksibenzaldehida s propargil-bromidom i kalijevim karbonatom kao bazom sintetiziran je 4-metoksi-3-(prop-2-in-1-iloksi)benzaldehid (15). Reakcijom kondenzacije spoja 15 i 2-aminotiofenola uz natrijev metabisulfit kao oksidacijsko sredstvo u dimetilformamidu pripravljen je 2-(4-metoksi-3-(prop-2-in-1-iloksi)fenil)benzo[d]tiazol (16). 1,2,3-triazolni derivati benzotiazola (17-26) sintetizirani su mehanokemijskom Huisgenovom 1,3-dipolarnom cikloadicijom spoja 16 i odgovarajućih azida u metanolu uz bakrov(II) acetat kao katalizator. Strukturna karakterizacija priređenih spojeva provedena je spektroskopijom 1H i 13C-NMR. In silico analizom predviđeni su farmakološki učinci i moguće biološke mete pripravljenih spojeva.In this paper, the synthesis of targeted benzothiazole derivatives bridged with a hydrazone coupling (3-14) and 1,2,3-triazole benzothiazole derivatives (17-26) as potentially biologically active agents is described, and their structural characterization by NMR spectroscopy was carried out. 2-amino-6-methoxybenzo[d]thiazole (1) was synthesized by the cyclization reaction of pmethoxyaniline with potassium thiocyanate and bromine in acetic acid, which was then converted into 2-hydrazinyl-6-methoxybenzo[d]thiazole (2) by reaction of nucleophilic substitution with hydrazine hydrate in the presence of ethylene glycol and hydrochloric acid. Benzothiazole hydrazone derivatives (3-14) were prepared by mechanochemical reactions of 2-hydrazinyl-6-methoxybenzo[d]thiazole (2) and corresponding aldehydes. 4-methoxy-3-(prop-2-yn-1-yloxy)benzaldehyde (15) was synthesized by microwave-assisted reaction of O-alkylation of 3-hydroxy-4-methoxybenzaldehyde with propargyl bromide and potassium carbonate as a base. 2-(4-methoxy-3-(prop-2-yn-1-yloxy)phenyl)benzo[d]thiazole (16) was prepared by the condensation reaction of compound 15 and 2-aminothiophenol with sodium metabisulfite as an oxidizing agent in dimethylformamide. 1,2,3-triazole derivatives of benzothiazole (17-26) were synthesized by mechanochemical Huisgen 1,3-dipolar cycloaddition of compound 16 and the corresponding azides in methanol with copper(II) acetate as a catalyst. Structural characterization of the prepared compounds was performed by 1H and 13C-NMR spectroscopy. Pharmacological effects and possible biological targets of the prepared compounds were predicted by in silico analysis
Synthesis, structural characterization and antibacterial activity of novel 2-hydrazone derivatives of benzothiazole
No full textU ovom radu opisana je sinteza ciljanih derivata benzotiazola premoštenih hidrazonskom spojnicom (3-14) i 1,2,3-triazolnih derivata benzotiazola (17-26) kao potencijalno biološki aktivnih agenasa te je provedena njihova strukturna karakterizacija spektroskopijom NMR. 2-amino-6-metoksibenzo[d]tiazol (1) sintetiziran je reakcijom ciklizacije p-metoksianilina s kalijevim tiocijanatom i bromom u octenoj kiselini koji je potom reakcijom nukleofilne supstitucije s hidrazin hidratom u prisustvu etilen-glikola i klorovodične kiseline preveden u 2-hidrazinil-6-metoksibenzo[d]tiazol (2). Benzotiazolni derivati hidrazona (3-14) pripremljeni su mehanokemijskim reakcijama 2-hidrazinil-6-metoksibenzo[d]tiazola (2) i odgovarajućih aldehida. Mikrovalovima potpomognutom reakcijom O-alkiliranja 3-hidroksi-4-metoksibenzaldehida s propargil-bromidom i kalijevim karbonatom kao bazom sintetiziran je 4-metoksi-3-(prop-2-in-1-iloksi)benzaldehid (15). Reakcijom kondenzacije spoja 15 i 2-aminotiofenola uz natrijev metabisulfit kao oksidacijsko sredstvo u dimetilformamidu pripravljen je 2-(4-metoksi-3-(prop-2-in-1-iloksi)fenil)benzo[d]tiazol (16). 1,2,3-triazolni derivati benzotiazola (17-26) sintetizirani su mehanokemijskom Huisgenovom 1,3-dipolarnom cikloadicijom spoja 16 i odgovarajućih azida u metanolu uz bakrov(II) acetat kao katalizator. Strukturna karakterizacija priređenih spojeva provedena je spektroskopijom 1H i 13C-NMR. In silico analizom predviđeni su farmakološki učinci i moguće biološke mete pripravljenih spojeva.In this paper, the synthesis of targeted benzothiazole derivatives bridged with a hydrazone coupling (3-14) and 1,2,3-triazole benzothiazole derivatives (17-26) as potentially biologically active agents is described, and their structural characterization by NMR spectroscopy was carried out. 2-amino-6-methoxybenzo[d]thiazole (1) was synthesized by the cyclization reaction of pmethoxyaniline with potassium thiocyanate and bromine in acetic acid, which was then converted into 2-hydrazinyl-6-methoxybenzo[d]thiazole (2) by reaction of nucleophilic substitution with hydrazine hydrate in the presence of ethylene glycol and hydrochloric acid. Benzothiazole hydrazone derivatives (3-14) were prepared by mechanochemical reactions of 2-hydrazinyl-6-methoxybenzo[d]thiazole (2) and corresponding aldehydes. 4-methoxy-3-(prop-2-yn-1-yloxy)benzaldehyde (15) was synthesized by microwave-assisted reaction of O-alkylation of 3-hydroxy-4-methoxybenzaldehyde with propargyl bromide and potassium carbonate as a base. 2-(4-methoxy-3-(prop-2-yn-1-yloxy)phenyl)benzo[d]thiazole (16) was prepared by the condensation reaction of compound 15 and 2-aminothiophenol with sodium metabisulfite as an oxidizing agent in dimethylformamide. 1,2,3-triazole derivatives of benzothiazole (17-26) were synthesized by mechanochemical Huisgen 1,3-dipolar cycloaddition of compound 16 and the corresponding azides in methanol with copper(II) acetate as a catalyst. Structural characterization of the prepared compounds was performed by 1H and 13C-NMR spectroscopy. Pharmacological effects and possible biological targets of the prepared compounds were predicted by in silico analysis
Synthesis and structural characterization of novel benzothiazole derivatives
No full textU ovom radu opisana je sinteza novih derivata benzotiazola primjenom mikrovalovima potpomognutih, mehanokemijskih i klik reakcija. Za sintezu derivata benzotiazola pripravljen je 4-O-propargilbenzaldehid (1) SN2 reakcijom 4-hidroksibenzaldehida i propargil-bromida uz K2CO3 kao bazu. 2-(4-(prop-2-in-1-iloksi)fenil)benzotiazol (2) priređen je ciklizacijom
4-O-propargilbenzaldehida (1) i 2-aminotiofenola u dimetilformamidu uz Na2S2O5 kao oksidacijsko sredstvo. Huisgenovom 1,3-dipolarnom cikloadicijom
2-(4-(prop-2-in-1-iloksi)fenil)benzotiazola (2) i odgovarajućih azida uz bakrov(II) acetat kao katalizator sintetizirani su 1,2,3-triazolni derivati benzotiazola (3-9). Mehanokemijske reakcije ciljanih derivata benzotiazola (3-9) provedene su u kugličnom mlinu. 1H i 13C-NMR spektroskopijom potvrđene su strukture svih novopripravljenih derivata benzotiazola.This paper describes the synthesis of new benzothiazole derivatives using microwaveassisted, mechanochemical and click reactions. For the synthesis of benzothiazole derivatives, 4-O-propargylated benzaldehyde (1) was prepared by SN2 reaction of 4-hydroxybenzaldehyde and propargyl bromide using K2CO3 as a base.
2-(4-(prop-2-yn-1-yloxy)phenyl) benzothiazole (2) was prepared by cyclization reaction of 4-O-propargyl benzaldehyde (1) and 2-aminothiophenol in dimethylformamide with Na2S2O5 as oxidizing agent. 1,2,3-triazolyl derivatives of benzothiazole (3-9) were prepared by Huisgen 1,3-dipolar cycloaddition of 2-4-(prop-2-yn-1-yloxy)phenyl benzothiazole (2) and the corresponding azides using copper(II) acetate as catalyst. Mechanochemical reactions of the desired compounds (3-9) were performed in a ball mill. The structures of all newly prepared benzothiazole derivatives were confirmed by 1H and 13C-NMR spectroscopy
Going Beyond Counting First Authors in Author Co-citation Analysis
Get PDFThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
Get PDF“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Get PDFWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
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