- INFLUENZA VIRUS REPLICATION INHIBITOR AND USE THEREOF
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Disclosed are a compound as shown in formula (I) as an influenza virus replication inhibitor and a preparation method therefor, a pharmaceutical composition comprising the compound and the use of the compound and pharmaceutical composition thereof in the treatment of influenza.
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- Cobalt-Catalyzed Direct C-H Thiolation of Aromatic Amides with Disulfides: Application to the Synthesis of Quetiapine
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A direct C(sp2)-H thiolation of aromatic amides with disulfides was developed. The coupling reaction proceeds between the thioether radical and cobaltacycle intermediate. This method exhibits a relatively broad substrate scope and high functional group compatibility. A mechanistic study indicates that the cobalt(IV) intermediate is probably formed during the course of the reaction. The thiolation product can be transformed to Quetiapine, which is an atypical antipsychotic agent approved for the treatment of schizophrenia and bipolar disorder.
- Li, Mingliang,Wang, Jun Joelle
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p. 6490 - 6493
(2018/10/20)
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- Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives
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Novel N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives were designed, synthesized and their chemical structures were confirmed by 1H NMR, 13C NMR and Mass spectra. The anticancer activities of the newly synthesized compounds were evaluated in vitro against three human cancer cell lines including K562, Colo-205 and MDA-MB 231 by MTT assay. The screening results showed that five compounds (16b, 16d, 16i, 16p and 16q) exhibited potent cytotoxic activities with IC50 values between 20 and 40 μM. Further in vitro studies revealed that inhibition of sirtuins could be the possible mechanism of action of these molecules.
- Gudisela, Mura Reddy,Srinivasu,Mulakayala, Chaitanya,Bommu, Praveen,Rao, M.V. Basaveswara,Mulakayala, Naveen
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p. 4140 - 4145
(2017/08/23)
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- MOISTURE-STABLE HOLOGRAPHIC MEDIA
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The invention relates to novel compounds which are especially suitable for use as writing monomers in holographic media. The invention further provides a photopolymer and a holographic medium comprising the inventive compounds, and an optical display, a security document and a holographic optical element comprising an inventive holographic medium.
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Paragraph 0185
(2018/01/18)
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- Synthesis, characterization and antimicrobial activity of 2-(11-oxodibenzo [b,f][1,4]thiazepin-10(11H)-yl)-N (substituted phenyl) acetamide derivatives
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Substituted dibenzo [b,f][1,4]thiazepines analogues carrying 2-chloro N-phenylacetamide moiety attached to 11-C position have been synthesized and evaluated using IR, 1H NMR and mass spectra. Antibacterial properties have been examined for the synthesized derivatives against gram positive and gram negative bacteria. 2-(11-Oxodibenzo [b,f][1,4]thiazepin-10(11H)-yl)-N phenylacetamide derivatives show good significant antimicrobial activity.
- Tailor, Jitesh H.,Patel, Priti C.,Malik
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p. 1263 - 1268
(2014/12/10)
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- Diversified synthesis of novel quinoline and dibenzo thiazepine derivatives using known active intermediates
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The novel drug development to control resisting infections in conventional drug therapy is a need of today. Few antiulcer relative derivatives developed by approaching convergent synthesis. The derivatives synthesized successfully are dibenzo thiazepine-pyridine (SLN11-SLN15) and benzimidazole-hydroquinoline based derivatives (SLN16-SLN20). It involved the coupling through microwave, sonication and conventional techniques at final step. The efficient technology identified as sonication technique basically time and yield. The reported compounds were structural characterized by elemental analysis and spectral studies such as 1H, 13C NMR and MS.
- Sharada,Satyanarayana Reddy,Sammaiah,Sumalatha
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p. 7959 - 7966
(2013/09/23)
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- PROCESS FOR PREPARATION OF DIBENZOTHIAZEPINONE COMPOUNDS
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The present invention discloses a process for the preparation of dibenzothiazepinone compounds of Formula I. The process for preparation of a dibenzothiazepinone compound of Formula I comprises reaction of compound of formula II in the presence of an acid catalyst comprising phosphorus pentoxide and methanesulfonic acid. The dibenzothiazepinone compounds of Formula I are key intermediate for the preparation of 2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol known as quetiapine and its derivatives, which are effective antipsychotic substances.
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Page/Page column 9
(2011/10/13)
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- Synthesis and antibacterial activities of new dibenzothiazepine derivatives
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A number of substituted dibenzo[b,f][1,4]thiazepines analogues carrying heterocyclic and aliphatic moiety attached to C-11 position have been synthesized and evaluated their antibacterial activities against gram positive and gram negative bacteria. Derivatives of imidazole, 2-methyl imidazole and pyrrolidine exhibit significant antibacterial activities.
- Mahale, Ganesh D.,Kolekar, Yogesh M.,Kumar, Ashok,Singh, Dharmendra,Kodam, Kisan M.,Waghmode, Suresh B.
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scheme or table
p. 1196 - 1201
(2011/10/12)
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- PROCESS FOR THE PREPARATION OF 11-(1-PIPERAZINYL)DIBENZO `B, F! `1 ,4!-THIAZEPINE, AN INTERMEDIATE IN THE SYNTHESIS OF THE ANTIPSYCHOTIC DRUG QUETIAPINE
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A process for the preparation of 11-(1-piperazinyl)dibenzo-[b, f ] [ 1, 4 ] thiazepine comprising reacting phenyl 2-(phenylthio) phenylcarbamate with piperazine and cyclizing the obtained N-[ (2 -phenylthio) phenyl ] -1 -piperazinylcarboxamide in a presence of cyclizing agent. 11-(1-piperazinyl)-dibenzo [b, f] [1, 4]thiazepine is itself, an intermediate in the synthesis of antipsychotic drug Quetiapine.
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Page/Page column 6-8; 12
(2008/06/13)
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