63638-85-7Relevant academic research and scientific papers
Practical, Large-Scale Preparation of Benzoxepines and Coumarins through Rhodium(III)-Catalyzed C-H Activation/Annulation Reactions
Gulías, Moisés,Marcos-Atanes, Daniel,Mascare?as, José L.,Font, Marc
supporting information, p. 1669 - 1673 (2019/09/04)
Herein we disclose the assembly of benzoxepines and coumarins from 2-alkenylphenol precursors using [Cp*RhCl2]2 as the precatalyst and alkynes or carbon monoxide as reacting partners. The preparation of benzoxepines and coumarins can be scaled up to 33 mmol using low catalyst loadings.
3-(Triflyloxy)benzynes Enable the Regiocontrolled Cycloaddition of Cyclic Ureas to Synthesize 1,4-Benzodiazepine Derivatives
Kaneko, Hideki,Ikawa, Takashi,Yamamoto, Yuta,Arulmozhiraja, Sundaram,Tokiwa, Hiroaki,Akai, Shuji
supporting information, p. 943 - 948 (2018/02/26)
A versatile synthesis of 1,4-benzodiazepine derivatives through the reaction of various 3-(trifluoromethanesulfonyloxy)benzynes with N -(p -toluenesulfonyl)imidazolidin-2-ones is reported. This reaction system provides a 1,4-benzodiazepine bearing a trifluoromethanesulfonyloxy group as a single regioisomer among the four possible regioisomers.
ANTIBACTERIAL AGENT
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Paragraph 0112; 0117; 0118, (2015/11/30)
An antibacterial agent comprising a compound represented by the following general formula (I), which can exhibit potent antibacterial activity against bacteria that have acquired resistance to quinolones (in the formula, R1 and R4 re
Design, synthesis and anticancer properties of 5-arylbenzoxepins as conformationally restricted isocombretastatin A-4 analogs
Rasolofonjatovo, Evelia,Provot, Olivier,Hamze, Abdallah,Rodrigo, Jordi,Bignon, Jerome,Wdzieczak-Bakala, Joanna,Lenoir, Christine,Desravines, Deborah,Dubois, Joelle,Brion, Jean-Daniel,Alami, Mouad
, p. 28 - 39 (2013/05/09)
A series of novel benzoxepins 6 was designed and prepared as rigid-isoCA-4 analogs according to a convergent strategy using the coupling of N-tosylhydrazones with aryl iodides under palladium catalysis. The most potent compound 6b, having the greatest resemblance to CA-4 and isoCA-4 displayed antiproliferative activity at nanomolar concentrations against various cancer cell lines and inhibited tubulin assembly at a micromolar range. In addition, benzoxepin 6b led to the arrest of HCT116, K562, H1299 and MDA-MB231 cancer cell lines in the G2/M phase of the cell cycle, and strongly induced apoptosis at low concentrations. Docking studies demonstrated that benzoxepin 6b adopt an orientation similar to that of isoCA-4 at the colchicine binding site on β-tubulin.
Synthesis of 8-aryl-substituted coumarins based on ring-closing metathesis and Suzuki-Miyaura coupling: Synthesis of a furyl coumarin natural product from Galipea panamensis
Schmidt, Bernd,Krehl, Stefan,Kelling, Alexandra,Schilde, Uwe
supporting information; experimental part, p. 2360 - 2367 (2012/05/31)
The synthesis of 7-methoxy-8-(4-methyl-3-furyl)-2H-chromen-2-one, a natural product with antileishmanial activity recently isolated from the plant Galipea panamensis, is described. The key step is a Suzuki-Miyaura coupling of a furan-3-boronic acid and an
Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal
Pereira, Alban R.,Strangman, Wendy K.,Marion, Frederic,Feldberg, Larry,Roll, Deborah,Mallon, Robert,Hollander, Irwin,Andersen, Raymond J.
supporting information; experimental part, p. 8523 - 8533 (2011/02/26)
Analogues of the sponge meroterpenoid liphagal (1) have been synthesized and evaluated for inhibition of PI3Kα and PI3Kα as part of a program aimed at developing new isoform-selective PI3K inhibitors. One of the analogues, compound 24, with IC50/sub
Antiangiogenic versus cytotoxic activity in analogues of aeroplysinin-1
Cordoba, Ruben,Tormo, Nelida Salvador,Medarde, Antonio Fernandez,Plumet, Joaquin
, p. 5300 - 5315 (2008/03/13)
A series of analogues of the potentially angiogenic inhibitor aeroplysinin-1 1 were synthesized and their in vitro antiangiogenic and cytotoxic activities evaluated. In the case of epoxy ketone 6 and azlactone 36 the relationship sprouting inhibition assay/cytotoxicity in BAE cells was enhanced by one order and two orders of magnitude, respectively, with respect to the reference. These results imply more specific antiangiogenic properties for the synthesized derivatives.
Functionalized stilbene derivatives as improved vascular targeting agents
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, (2008/06/13)
Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compound
SYNTHESIS OF N-SUCCINIMIDYL-2,4-DIMETHOXY-3-(TRI-N-BUTYLSTANNYL) BENZOATE VIA REGIO-SPECIFICALLY GENERATED LITHIUM 2,4-DIMETHOXY-3-LITHIOBENZOATE
Narula, Acharan S.,Zalutsky, Michael R.
, p. 4385 - 4388 (2007/10/02)
Lithium 2,4-dimethoxy-3-lithiobenzoate can be efficiently generated from 2,4-dimethoxy-3-bromobenzoic acid in THF at -100 deg C.
