45438-73-1Relevant articles and documents
Identification of intermediates in the reaction of 2-thenyl halides with magnesium
Egorov,Kuznetsova,Anisimov
, p. 1544 - 1547 (2000)
The reaction of 2-thenyl chloride with magnesium was shown by the ESR method to proceed via the intermediate formation of radicals and radical ion pairs, whereas similar reactions of 2-thenyl bromide and iodide occur through the formation of free radicals only.
Optimization of interactions in crystal packing revealed by crystal structures [ethyl 2-(formylamino)-3-thien-2-yl-2-(thien-2-ylmethyl)propanoate and ethyl 3-(5-bromothien-2-yl)-2-[(5-bromothien-2-yl)methyl]-2-(formylamino) propanoate]
Damodharan, Lakshminarasimhan,Pattabhi, Vasantha,Behera, Manoranjan,Kotha, Sambasivarao
, p. 101 - 106 (2004)
The title compounds, C15H14NO3S 2 (I) and C15H15Br2NO 3S2 (II), are derivatives of Aib (α-aminoisobutyric acid) with thiophene rings substituted at the Cα position. The Cα substitution causes the backbone to assume an extended conformation in the crystal structure. N-H and C-H donors share the thiophene ring π system for X-H?π interactions. The packings of the molecules are stabilized by intermolecular N-H?O, C-H?O, C-H?π and C-H?Br hydrogen bonds. Br?O interactions and a weak dihydrogen bond have also been observed in the crystal structure of II. The packing adopted by II has maximized the number of interactions that are possible.
Synthesis and pharmacological characterisation of arctigenin analogues as antagonists of AMPA and kainate receptors
Butts, Craig P.,Collingridge, Graham L.,Jane, David E.,Mallah, Shahida,Molnár, Elek,Re?nik, Lisa-Maria,Thatcher, Robert J.,Willis, Christine L.
supporting information, p. 9154 - 9162 (2021/11/16)
(-)-Arctigenin and a series of new analogues have been synthesised and then tested for their potential as AMPA and kainate receptor antagonists of human homomeric GluA1 and GluK2 receptors expressed in HEK293 cells using a Ca2+ influx assay. In general, these compounds showed antagonist activity at both receptors with greater activity evident at AMPARs. Schild analysis indicates that a spirocyclic analogue 6c acts as a non-competitive antagonist. Molecular docking studies in which 6c was docked into the X-ray crystal structure of the GluA2 tetramer suggest that (-)-arctigenin and its analogues bind in the transmembrane domain in a similar manner to the known AMPA receptor non-competitive antagonists GYKI53655 and the antiepileptic drug perampanel. The arctigenin derivatives described herein may serve as novel leads for the development of drugs for the treatment of epilepsy. This journal is
Synthetic process of tiaprofenic acid
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Paragraph 0044; 0045, (2018/04/01)
The invention relates to a synthetic process of tiaprofenic acid. The synthetic process comprises the following steps: adopting 2-thiotolene as a starting raw material, enabling 2-thiotolene to reactwith trimethylsilyl cyanide to synthesize 2-thiopheneacetonitrile by virtue of bromation, then enabling the 2-thiopheneacetonitrile to react with dimethyl carbonate to be methylated, hydrolyzing cyanogroups, and finally performing F-K reaction with benzoyl chloride, and preparing tiaprofenic acid. The synthetic process has the advantages that the conventional safe raw materials low in price are used for substituting the rare expensive and dangerous raw materials, so that the severe pollution problem is avoided, and the production cost is greatly decreased; and in addition, the process route adopted by the invention is simple, the reaction period is short, the reaction condition is stable, the yield is high and can reach more than 90 percent, the produce obtained after the reaction is highin purity, and the purity can reach more than 99 percent, so that the synthetic process is suitable for the industrialized production.
