26086-61-3Relevant academic research and scientific papers
Synthesis, characterization and application of β-cyclodextrin-silica nanocomposite as potential microvessel in nucleophilic substitution reaction of phenacyl halides
Kiasat, Ali Reza,Nazari, Simin
, p. 429 - 438 (2013)
In the present study, β-cyclodextrin-silica hybrid is synthesized as a novel, efficient and eco-friendly microvessel and solid-liquid phase-transfer catalyst. This molecular host system was applied for nucleophilic substitution reaction of phenacyl halide
Indole-linked 1,2,3-triazole derivatives efficiently modulate COX-2 protein and PGE2 levels in human THP-1 monocytes by suppressing AGE-ROS-NF-kβ nexus
Aslam, Tooba,Basha, Fatima Z.,Choudhary, M. Iqbal,Iqbal, Shazia,Jahan, Humera,Khan, Maria Aqeel,Siddiqui, Nimra Naz
, (2022/01/19)
Aims: AGEs augment inflammatory responses by activating inflammatory cascade in monocytes, and hence lead to vascular dysfunction. The current study aims to study a plausible role and mechanism of a new library of indole-tethered 1,2,3-triazoles 2-13 in A
Synthesis of Novel Heterocycles by Amide Activation and Umpolung Cyclization
Maulide, Nuno,Riomet, Margaux,Roller, Alexander,Zhang, Haoqi
supporting information, (2020/03/24)
Herein, we report a metal-free synthesis of cyclic amidines, oxazines, and an oxazinone under mild conditions by electrophilic amide activation. This strategy features an unusual Umpolung cyclization mode and enables the smooth union of α-aryl amides and diverse alkylazides, effectively rerouting our previously reported α-amination transform.
Carbon isotope labeling of carbamates by late-stage [11C], [13C] and [14C]carbon dioxide incorporation
Del Vecchio, Antonio,Talbot, Alex,Caillé, Fabien,Chevalier, Arnaud,Sallustrau, Antoine,Loreau, Olivier,Destro, Gianluca,Taran, Frédéric,Audisio, Davide
supporting information, p. 11677 - 11680 (2020/10/19)
A general procedure for the late-stage [11C], [13C] and [14C]carbon isotope labeling of cyclic carbamates is reported. This protocol allows the incorporation of carbon dioxide, the primary source of carbon-14 and carbon-11 radioisotopes, in a direct, cost-effective and sustainable manner. A disconnection/reconnection strategy, involving ring opening/isotopic closure, was also implemented.
Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents
Bangalore, Pavan K.,Vagolu, Siva K.,Bollikanda, Rakesh K.,Veeragoni, Dileep K.,Choudante, Pallavi C.,Misra, Sunil,Sriram, Dharmarajan,Sridhar, Balasubramanian,Kantevari, Srinivas
supporting information, p. 26 - 35 (2020/01/03)
(+)-Usnic acid, a product of secondary metabolism in lichens, has displayed a broad range of biological properties such as antitumor, antimicrobial, antiviral, anti-inflammatory, and insecticidal activities. Interested by these pharmacological activities and to tap into its potential, we herein present the synthesis and biological evaluation of new usnic acid enaminone-conjugated 1,2,3-triazoles 10-44 as antimycobacterial agents. (+)-Usnic acid was condensed with propargyl amine to give usnic acid enaminone 8 with a terminal ethynyl moiety. It was further reacted with various azides A1-A35 under copper catalysis to give triazoles 10-44 in good yields. Among the synthesized compounds, saccharin derivative 36 proved to be the most active analogue, inhibiting Mycobacterium tuberculosis (Mtb) at an MIC value of 2.5 μM. Analogues 16 and 27, with 3,4-difluorophenacyl and 2-acylnaphthalene units, respectively, inhibited Mtb at MIC values of 5.4 and 5.3 μM, respectively. Among the tested Gram-positive and Gram-negative bacteria, the new derivatives were active on Bacillus subtilis, with compounds 18 [3-(trifluoromethyl)phenacyl] and 29 (N-acylmorpholinyl) showing inhibitory concentrations of 41 and 90.7 μM, respectively, while they were inactive on the other tested bacterial strains. Overall, the study presented here is useful for converting natural (+)-usnic acid into antitubercular and antibacterial agents via incorporation of enaminone and 1,2,3-triazole functionalities.
Photocatalyst-Free Visible-Light Enabled Synthesis of Substituted Pyrroles from α-Keto Vinyl Azides
Borra, Satheesh,Borkotoky, Lodsna,Newar, Uma Devi,Das, Babulal,Maurya, Ram Awatar
supporting information, p. 3364 - 3368 (2020/07/13)
An efficient photocatalyst-free visible light enabled synthesis of substituted pyrroles from α-keto vinyl azides (readily prepared via Knoevenagel condensation of phenacyl azides with 2-oxo-2H-chromene-3-carbaldehydes) was developed. The reaction proceeds
Imidazolium-Based Ionic Network as a Robust Heterogeneous Catalyst in Synthesis of Phenacyl Derivatives
Kakesh,Sayyahi,Badri,Tahanpesar
, p. 1218 - 1220 (2019/07/16)
A new imidazolium-based poly(ionic liquid) has been synthesized and used as a robust heterogeneous catalyst for the preparation of phenacyl derivatives by an SN2 reaction of different phenacyl bromides with a broad range of nucleophiles. The products are obtained in high yields under mild conditions. The catalyst can be recycled efficiently.
Facile synthesis of 1,2,3-triazole-fused indolo- and pyrrolo[1,4]diazepines, DNA-binding and evaluation of their anticancer activity
Gour, Jitendra,Gatadi, Srikanth,Pooladanda, Venkatesh,Ghouse, Shaik Mahammad,Malasala, Satyaveni,Madhavi,Godugu, Chandraiah,Nanduri, Srinivas
supporting information, (2019/10/05)
A facile synthetic strategy has been developed for the generation of structurally diverse N-fused heterocycles. The formation of fused 1,2,3-triazole indolo and pyrrolodiazepines proceeds through an initial Knoevenagel condensation followed by intramolecu
Preparation method of alpha-azide arone derivative
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Paragraph 0065-0067, (2019/06/12)
The invention relates to a preparation method of an alpha-azide arone derivative. The method comprises the steps that substituted styrene, azidotrimethylsilane and an oxidant are added into a Schlenkreaction flask, water is added to serve as a solvent, a
Synthesis of new bicarbazole-linked triazoles as non-cytotoxic reactive oxygen species (ROS) inhibitors
Iqbal, Shazia,Khan, Maria A.,Ansari, Zulqarnain,Jabeen, Almas,Faheem, Aisha,Fazal-Ur-Rehman, Saba,Basha, Fatima Z.
, p. 2330 - 2341 (2019/07/05)
Carbazole analogs 3 and 4 and a new library of bicarbazole-linked triazoles 6–11 were prepared via new synthetic methodology. Metal-catalyzed oxidative coupling reaction was utilized for the synthesis of bicarbazole acetylene 4 and different metals (Znsu
