- Novel 1,4-benzothiazine derivatives: synthesis, crystal structure, and anti-bacterial properties
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In order to develop relatively small molecules as pharmacologically active molecules, novel 1,4-benzothiazine derivatives with triazole and oxazolidinone were synthesized. In this study, a series of 1,2,3-triazolylmethyl-1,4-benzothiazine derivatives were developed by exploiting a click chemistry reaction using a CuI-catalyzed Huisgen [3?+?2] cycloaddition. Starting from 2-(substituted)-3,4-dihydro-2H-1,4-benzothiazi-3-one, a number of 1,4-benzothiazine derivatives were also synthesized using different alkylating agents to give a 4-(substituted)-2-(substituted)-3,4-dihydro-2H-1,4-benzothiazi-3-one in good yields. The crystal and molecular structure of compound oxazolidin-2-one in basic benzothiazine was established by single-crystal X-ray diffraction. The newly synthesized products were subjected to in vitro biological evaluation. The result indicated that the compounds show convincing antibacterial activities against different microorganisms. All structures of the synthesized compounds were elucidated on the basis of spectral analyses and chemical reactions.
- Sebbar, Nada Kheira,Mekhzoum, Mohamed El Mehdi,Essassi, El Mokhtar,Zerzouf, Abdelfettah,Talbaoui, Ahmed,Bakri, Youssef,Saadi, Mohamed,Ammari, Lahcen El
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- Copper-catalyzed highly selective synthesis of 2-benzyl- and 2-benzylidene-substituted benzo[: B] thiazinones from 2-iodophenylcinnamamides and potassium sulfide
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An efficient and practical procedure for the synthesis of 2-benzyl- and 2-benzylidene-substituted benzo[b]thiazinones from easily available 2-iodophenylcinnamamides and potassium sulfide has been developed. In the presence of DBU, the reaction proceeds vi
- Liu, Wenjuan,Min, Hao,Zhu, Xiaoming,Deng, Guobo,Liang, Yun
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p. 9804 - 9808
(2017/12/08)
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- Synergistic promoting effect of ball milling and KF–alumina support as a green tool for solvent-free synthesis of 2-arylidene-benzothiazinones
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A solvent-free procedure is developed for the reaction of benzothiazinones with benzaldehyde derivatives, where the solid KF–Al2O3 support and ball milling synergistically leads to a green and efficient synthesis of several 2-arylide
- Sharifi, Ali,Ansari, Mohammad,Darabi, Hossein Reza,Abaee, M. Saeed
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p. 593 - 600
(2016/12/03)
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- Rearrangements and Complex Eliminations with 1,5-Benzothiazepin-4-ones
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The 1,5-benzothiazepin-4-ones 3, 5, and 7 - 10 are pyrolyzed (with proton catalysis in part).New or rarely documented rearrangements and complex eliminations occur.These are classified and mechanistically discussed.The products and by-products are spectroscopically characterized (IR, UV, NMR, MS).Their configurations are elucidated via photolysis experiments. 4 photodimerizes in solution and in the crystalline state with great ease to give 14. 11 is remarkably insensitive towards hydrolysis.
- Kaupp, Gerd,Gruendken, Eleonore,Matthies, Doris
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p. 3109 - 3120
(2007/10/02)
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