76429-63-5Relevant academic research and scientific papers
Expedient Access to 2-Benzazepines by Palladium-Catalyzed C?H Activation: Identification of a Unique Hsp90 Inhibitor Scaffold
Virelli, Matteo,Moroni, Elisabetta,Colombo, Giorgio,Fiengo, Lorenzo,Porta, Alessio,Ackermann, Lutz,Zanoni, Giuseppe
, p. 16516 - 16520 (2018/10/25)
Bioactive 2-benzazepines were accessed in an atom- and step-economical manner through a versatile palladium-catalyzed C?H activation strategy. The C?H arylation required low catalyst loading and a mild base, which was reflected by a broad scope and high functional-group tolerance. The benzotriazolodiazepinones were identified as new heat shock protein 90 (Hsp90) inhibiting lead compounds, with considerable potential for anti-cancer applications.
An Efficient K2CO3-Promoted Synthesis of 1-Bromo-2-aryloxyethane Derivatives and Evaluation of Larval Mortality against Aedes aegypti
Pájaro, Yina,Sathicq, ángel,Puello-Polo, Esneyder,Pérez, Astrid,Romanelli, Gustavo,Trilleras, Jorge
, (2017/07/11)
The influences of reaction parameters on the etherification of phenols to obtain 1-bromo-2-aryloxyethane derivatives were evaluated. The compounds were prepared by direct etherification of phenols with 1,2-dibromoethane using anhydrous K2CO3 and acetonitrile as solvent reaction, at 80°C, in a reaction time of 6 h. Under these conditions, excellent yields (71%-94%) were obtained, with low yields of secondary products. The anhydrous K2CO3 was recycled by simple filtration, dried in vacuum, and reused. The compounds were characterized by conventional spectral data (MS and NMR). Larvicidal activity results showed a 100% larval mortality after 24-hour exposure to the compound 1-(2-bromoethoxy)-2-phenylbenzene.
CERTAIN PROTEIN KINASE INHIBITORS
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Paragraph 0631; 0632, (2014/05/20)
Disclosed herein are protein kinase inhibitors, more particu-larly novel pyrimidine derivatives and pharmaceutical com-positions thereof, and method of use thereof
Oxygen Heterocycles by the Parham Cyclialkylation
Bradsher, Charles K.,Reames, David C.
, p. 1384 - 1388 (2007/10/02)
The addition of butyllithium at -100 deg C to ω-bromoalkyl ethers of o-bromophenol (and its congeners) led to preferential exchange of the aryl bromine at position 2.The resulting organolithium reagents, under suitable conditions, cyclized to afford 2,3-dihydrobenzofurans (6), 3,4-dihydro-2H-1-benzopyrans (13), or 2,3,4,5-tetrahydro-1-benzoxepins (16) in good yields, but less satisfactory results were obtained with the intermediate expected to produce 8-methyl-3,4,5,6-tetrahydro-2H-1-benzoxocin (19). ω-Bromoethyl and ω-bromopropyl ethers of suitable dibromophenols were treated successively with 2 equiv of butyllithium and an electrophile to yield derivatives of 6 and 13.
