1898-85-7Relevant academic research and scientific papers
Expedient Pd-Catalyzed α-Arylation towards Dibenzoxepinones: Pivotal Manske's Ketone for the Formal Synthesis of Cularine Alkaloids
Deichert, Julie A.,Mizufune, Hideya,Patel, Jignesh J.,Hurst, Timothy E.,Maheta, Ashish,Kitching, Matthew O.,Ross, Avena C.,Snieckus, Victor
, p. 4693 - 4697 (2020/05/08)
The general synthesis of diversely substituted dibenzoxepinones by a combined Pd-catalyzed α-arylation and SNAr strategy is reported and applied to the synthesis of Manske's ketone, a key intermediate en route to the total synthesis of cularine alkaloids. In the course of this work, an unanticipated ring contraction reaction to a xanthone was observed and serves as a caveat for the conditions of the widely used α-arylation reaction.
Redox-Neutral α-Arylation of Alkyl Nitriles with Aryl Sulfoxides: A Rapid Electrophilic Rearrangement
Shang, Li,Chang, Yonghui,Luo, Fan,He, Jia-Ni,Huang, Xin,Zhang, Lei,Kong, Lichun,Li, Kaixiao,Peng, Bo
, p. 4211 - 4217 (2017/03/27)
A facile α-arylation of nitriles has been developed by simply introducing Tf2O and DABCO to the mixture of nitriles and aryl sulfoxides. The transformation consists of two sequential steps: (i) Tf2O-initiated electrophilic assembly a
ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME
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Paragraph 0247 - 0250, (2016/10/09)
The present invention relates to a novel compound represented by chemical formula 1, and an organic electroluminescent device comprising the same. The compound according to the present invention can improve light-emitting efficiency, driving voltage, and lifespan of the organic electroluminescent device by being used in an organic layer of the organic electroluminescent device.COPYRIGHT KIPO 2016
Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents
Boudhar, Aicha,Ng, Xiao Wei,Loh, Chiew Yee,Chia, Wan Ni,Tan, Zhi Ming,Nosten, Francois,Dymock, Brian W.,Tan, Kevin S.W.
, p. 231 - 249 (2016/05/24)
Malaria remains a significant infectious disease with even artemisinin-based therapies now facing resistance in the field. Development of new therapies is urgently needed, either by finding new compounds with unique modes of action, or by reversing resistance towards known drugs with 'chemosensitizers' or 'chemoreversal' agents (CRA). Concerning the latter, we have focused on the resistance mechanisms developed against chloroquine (CQ). We have synthesized a series of compounds related to previously identified CRAs, and found promising novel compounds. These compounds show encouraging results in a coumarin labeled chloroquine uptake assay, exhibiting a dose response in resensitising parasites to the antimalarial effects of chloroquine. Selected compounds show consistent potency across a panel of chloroquine and artemisinin sensitive and resistant parasites, and a wide therapeutic window. This data supports further study of CRAs in the treatment of malaria and, ultimately, their use in chloroquine-based combination therapies.
ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME
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Paragraph 0247-0250, (2016/10/08)
The present invention relates to a novel compound and an organic electroluminescent device comprising the same. The compound in accordance with the present invention is used in an organic material layer of the organic electroluminescent device, and thereby luminous efficiency, driving voltage, durability and other characteristics of an organic electroluminescent device can be improved.COPYRIGHT KIPO 2015
Synthesis of targeted dibenzo[b,f]thiepines and dibenzo[b,f]oxepines as potential lead molecules with promising anti-breast cancer activity
Ansari, Mohd. Imran,Arun, Ashutosh,Chakravarti, Bandana,Hajela, K.,Hussain, Mohd. Kamil,Konwar, Rituraj
supporting information, p. 113 - 124 (2020/12/04)
A targeted library of substituted dibenzo[b,f]thiepines and dibenzo[b,f]oxepines (prototypes I, II and III), and structurally analogous to tamoxifen have been synthesized as a new class of anti-breast cancer agents. All the prototype molecules exhibited potential antiproliferative activity against ER + ve and ER-ve breast cancer cell lines. Dibenzo[b,f]thiepine prototypes were found to be more active. Of all the compound tested, 14b exhibited potent in-vitro antiproliferative activity at 1.33 μM and 5 μM concentration in MCF-7 and MDA-MB-231 cell lines and was devoid of any cytotoxicity in normal HEK cells even at 50 μM. Cell cycle analysis showed that the compound 14b inhibited cell proliferation due to G0/G1 arrest in MCF-7 cells. Annexin-V FITC and PI staining experiments confirmed that the cell inhibition was primarily due to apoptosis and not by necrosis, which was also supported by LDH release assay experiment. Molecular docking studies showed better binding interaction of the new dibenzo[b,f]thiepine analogue 14b with the estrogen receptor (ER) as compared to 4-hydroxy-tamoxifen and this enhanced binding might be responsible for its estrogen antagonistic activity that induces cell cycle arrest, apoptosis and inhibition of breast cancer cells.
Synthesis of benzo-fused heterocycles by intramolecular α-arylation of ketone enolate anions
Guastavino, Javier F.,Rossi, Roberto A.
scheme or table, p. 460 - 472 (2012/03/11)
A two-step synthesis of six-, seven-, eight-, and nine-member benzo-fused heterocycles in good to excellent yields is reported. The synthetic strategy involves the generation of a new intramolecular α-aryl ketone bond by the photostimulated SRN1 reaction of ketone enolate anions linked to a pendant haloarene as the key step. On the other hand, an intramolecular C Ar-CAr coupling led to the formation of five- and six-member benzo-fused heterocycles (9H-carbazole and phenanthridine) when an aromatic amide anion is competitively formed.
SPIRO COMPOUNDS USEFUL AS ANTAGONISTS OF THE H1 RECEPTOR
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Page/Page column 37-38, (2009/03/07)
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
Ueber die Bildung von dibenzoanellierten Siebenring-Alkinen
Lorch, Margret,Meier, Herbert
, p. 2382 - 2391 (2007/10/02)
The multi-step preparations and the thermal and alkaline fragmentations of the 1,2,3-selenadiazoles 13 and 23 are described.The most interesting feature of this investigation is the formation of the highly strained cycloalkynes 4 and 5 which were trapped in situ.
