- New class of diethyl substituted phosphoramidimidates and phosphonimidates: synthesis, spectral characterization and antimicrobial activity
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A series of new class of diethyl N-2-hydroxyethyl-N'-substituted phosphoramidimidates 6(a–e) and diethyl P-morpholino-N-substituted phosphonimidates 6(f–j) was synthesized. The precursor intermediates, diethyl substituted phosphoramidites 3(a–b) were prepared initially by a reaction of various amines 1(a–b) and diethyl phosphorochloridite (2) and then they were treated by in situ with aromatic/alkyl azides through Staudinger reaction to accomplish title products. Structures of all the synthesized compounds were characterized by spectroscopic data such as IR, NMR (1H, 13C, 31P), mass, and elemental analyses. The synthesized compounds were screened for their in vitro antimicrobial activity to understand their biological potency. The biological screening results disclosed that compounds 6b, 6c, 6e, 6g, 6h and 6j having potent antimicrobial activity against all the tested pathogens.
- Varalakshmi, Mavallur,Nagaraju, Chamarthi,Krishna, Palaa
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- Optimizing the aryl-triazole of cjoc42 for enhanced gankyrin binding and anti-cancer activity
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Gankyrin is an oncoprotein overexpressed in numerous cancer types and appears to play a key role in regulating cell proliferation, cell growth, and cell migration. These roles are largely due to gankyrin's protein-protein interaction with the 26S proteaso
- Almasri, Joseph,D'Souza, Amber,Dukhande, Vikas V.,Farrales, Pamela,Gnanmony, Manu,Gupta, Vivek,Juang, Daniel,Kabir, Abbas,Kanabar, Dipti,Muth, Aaron,Shukla, Snehal,Torrents, Nicolas
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supporting information
(2020/07/10)
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- Glucose promoted facile reduction of azides to amines under aqueous alkaline conditions
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A quick and efficient method for the reduction of azides to amines in water using d-glucose and KOH as green reagents is reported. The protocol is simple, inexpensive, scalable, and can be applied to different aromatic, heteroaromatic and sulphonyl azides. A high level of chemoselectivity is observed for azide reduction in the presence of other reducible functionalities like cyano, nitro, ether, ketone, amide and acid. The reaction gets completed in a short time (5-20 minutes), and furnishes the amines in high yield (85-99%). Unlike conventional hydrogenations, this reduction protocol does not require any metal catalyst, elaborate experimental setup or use of high-pressure equipment.
- Chandna, Nisha,Kaur, Fatehjeet,Kumar, Shobhna,Jain, Nidhi
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supporting information
p. 4268 - 4271
(2017/09/29)
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- One pot synthesis of aromatic azide using sodium nitrite and hydrazine hydrate
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A simple, rapid, and efficient protocol for the synthesis of aryl azide using sodium nitrite and hydrazine hydrate at room temperature is discussed. The short reaction time, simple work-up procedure, and use of inexpensive reagents are advantages of this method.
- Siddiki, Afsar Ali,Takale, Balaram S.,Telvekar, Vikas N.
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p. 1294 - 1297
(2013/03/13)
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- Synthesis of 2-azido-1,3-thiazoles as 1,2,3-triazole precursors
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By diazotization of 2-aminothiazoles and reaction with sodium azide, the derivatives of 2-azidothiazole were synthesized. Conditions of diazotization were selected according to the nature of a substituent in thiazoles. 2-Azidothiazole derivatives were studied in the base-catalysed condensation reactions with activated methylenic compounds to yield new 1-(1,3-thiazol-2-yl)- 1H-1,2,3-triazole-4-carboxylic acids.
- Pokhodylo, Nazariy T.,Savka, Roman D.,Pidlypnyi, Nazar I.,Matiychuk, Vasyl S.,Obushak, Mykola D.
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experimental part
p. 391 - 399
(2010/03/30)
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- On the utility of the azido transfer protocol: Synthesis of 2- And 5-azido N-methylimidazoles, 1,3-thiazoles and N-methylpyrazole and their conversion to triazole - azole bisheteroaryls
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The azido transfer procedure of heteroaryllithium and tosyl azide was used to synthesize selected 2- and 5-azidoazoles. This procedure, which is based on the fragmentation of the appropriate lithium triazene salts 1a-7a, successfully afforded 2-azido-N-methylimidazole 1, 2-azido-l,3-thiazole 2, 2-azidobenzo-1.3-thiazole 3, 5-azido-N-methylpyrazole 4, 5-azido-N- methylimidazole 6 [via 2-(trimethylsilyl)-5-azido-N-methylimidazole 5], and 5-azido-l,3-thiazole 7 (via 5-lithio-1,3-thiazole), but attempts to prepare 5-azido-2-(trimethylsilyl)-1,3-thiazole 8 from the corresponding triazene 7a failed, affording only the desilylated azide 7 in poor yield. Azidcs 1-7 underwent 1,3-dipolar cycloaddition when mixed with neat (trimethylsilyl) acetylene, giving 1-heteroaryl-4-trimethylsilyl-1,2.3-triazoles 1b-7b generally in very high yields. The Royal Society of Chemistry 2005.
- Zanirato, Paolo,Cerini, Stefano
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p. 1508 - 1513
(2007/10/03)
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