125259-03-2Relevant academic research and scientific papers
Synthesis of novel isoflavone/benzo-δ-sultam hybrids as potential anti-inflammatory drugs
Mengheres, Gabriel,Rice, Craig R.,Olajide, Olumayokun A.,Hemming, Karl
supporting information, (2021/01/12)
A small series of novel isoflavone/benzo-δ-sultam hybrids was synthesised and evaluated as potential anti-inflammatory and neuroprotective drugs in LPS-activated BV2 microglia. The benzo-δ-sultam core was constructed in a two-step reaction by coupling 2-halobenzenesulfonamide derivatives with terminal alkynes, followed by a 6-endo-dig cyclisation. The synthesised compounds, including precursors and hybrids, were tested for their ability to inhibit NO and TNF-α production in LPS-stimulated BV2 microglial cells, and the results are promising. The most potent hybrid reduces the NO production to 41%, and the TNF-α to 34% at 20 μM final concentration in the well.
Functionalization of α-C(sp3)?H Bonds in Amides Using Radical Translocating Arylating Groups
Radhoff, Niklas,Studer, Armido
supporting information, p. 3561 - 3565 (2021/01/04)
α-C?H arylation of N-alkylamides using 2-iodoarylsulfonyl radical translocating arylating (RTA) groups is reported. The method allows the construction of α-quaternary carbon centers in amides. Various mono- and disubstituted RTA-groups are applied to the arylation of primary, secondary, and tertiary α-C(sp3)?H-bonds. These radical transformations proceed in good to excellent yields and the cascades comprise a 1,6-hydrogen atom transfer, followed by a 1,4-aryl migration with subsequent SO2 extrusion.
AgNO3 mediated C-N bond forming reaction: Synthesis of 3-substituted benzothiazines as potential COX inhibitors
Rambabu, D.,Murthy, P. V. N. S.,Prasad, K. R. S.,Kandale, Ajit,Deora, Girdhar Singh,Pal, Manojit,Basaveswara Rao, M. V.
supporting information, p. 6577 - 6583,7 (2012/12/11)
AgNO3 facilitated the intramolecular ring closure of o-(1-alkynyl)benzenesulfonamides via a regioselective C-N bond forming reaction leading to the formation of 3-substituted benzothiazine derivatives. A number of compounds were prepared in goo
AgNO3 mediated C-N bond forming reaction: Synthesis of 3-substituted benzothiazines as potential COX inhibitors
Rambabu,Murthy,Prasad,Kandale, Ajit,Deora, Girdhar Singh,Basaveswara Rao,Pal, Manojit
supporting information, p. 6577 - 6583 (2013/01/15)
AgNO3 facilitated the intramolecular ring closure of o-(1-alkynyl)benzenesulfonamides via a regioselective C-N bond forming reaction leading to the formation of 3-substituted benzothiazine derivatives. A number of compounds were prepared in goo
3-Mercaptopropionic Acid: A New Tool in the Synthesis of Symmetrical Diaryl Sulfides from Unactivated Aryl Iodides as Substitute for Anhydrous Sodium Sulfide
Rabai, Jozsef
, p. 523 - 525 (2007/10/02)
A series of symmetrical diaryl sulfides has been prepared by the copper-catalyzed reaction of 3-mercaptopropionic acid with unactivated aryl iodides.The yields are comparable with those obtained using anhydrous sodium sulfide under optimized reaction conditions.
