Regioselective One-Pot Synthesis, Biological Activity and Molecular Docking Studies of Novel Conjugates N-(p-Aryltriazolyl)-1,5-benzodiazepin-2-ones as Potent Antibacterial and Antifungal Agents [PDF]
Novel 1,2,3-triazolo-linked-1,5-benzodiazepinones were designed and synthesized via a Cu(I)-catalyzed 1,3-dipolar alkyne-azide coupling reaction (CuAAC).
Asma Nsira +5 more
doaj +2 more sources
A novel Pd-catalysed sequential carbonylation/cyclization approach toward bis-N-heterocycles: rationalization by electronic structure calculations [PDF]
An unprecedented palladium-catalysed sequential aminocarbonylation/cyclization synthetic strategy, using carbon monoxide and structurally different aliphatic diamines as N-nucleophiles, gives access, in one pot, to a new family of indole-based N ...
Liliana Damas +6 more
doaj +2 more sources
Regioselective Halogenation of 1,4-Benzodiazepinones via CH Activation. [PDF]
AbstractThis article reports an efficient CH activation process for regioselective halogenation of 1,4-benzodiazepinones. Direct halogenation with NXS (X = Br, I) affords halogenated benzodiazepinones on the central aromatic ring whereas catalyst (Pd(OAc)2) controlled CH activation furnishes regioselectively ortho halogenated benzodiazepinones on the ...
Abdelkafi H, Cintrat JC.
europepmc +5 more sources
Structure of 1,5-benzodiazepinones in the solid state and in solution: Effect of the fluorination in the six-membered ring [PDF]
Two novel tetrafluorinated 1,5-benzodiazepinones were synthesized and their X-ray structures determined. 6,7,8,9-Tetrafluoro-4-methyl-1,3-dihydro-2H-1,5-benzodiazepin-2-one crystallizes in the monoclinic P21/c space group and 6,7,8,9-tetrafluoro-1,4 ...
Marta Pérez-Torralba +7 more
doaj +2 more sources
Benzodiazepinone Derivatives as CRTH2 Antagonists. [PDF]
Multiple CRTH2 antagonists are currently evaluated in human clinical trials for asthma and chronic obstructive pulmonary disease (COPD). During our lead optimization for CRTH2 antagonists, an observation of an intramolecular hydrogen bond in ortho-phenylsulfonamido benzophenone derivatives led to the design and synthesis of conformationally constrained
Liu JJ, Cheng AC, Tang HL, Medina JC.
europepmc +4 more sources
Copper-promoted synthesis of 1,4-benzodiazepinones via alkene diamination. [PDF]
A new method for the synthesis of 2-aminomethyl functionalized 1,4-benzodiazepin-5-ones is presented. The benzodiazepine core is well-known to interact with biological receptors and many pharmaceutical drugs are derived from this structure. The alkene diamination strategy is employed for the first time for the synthesis of 1,4-benzodiazepinones.
Karyakarte SD +6 more
europepmc +4 more sources
Challenging Atroposelective C–H Arylation
Atropisomeric molecules are privileged scaffolds, not only as ligands for asymmetric synthesis, but also as biologically active products and advanced materials.
Joanna Wencel-Delord +1 more
doaj +1 more source
(4Z)-1-Propargyl(1,3-Dipropargyl)-4-(2-oxopropylidene)-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one
n ...
Ould Mohamed Sidya Mohamed Said +6 more
doaj +1 more source
(4Z)-1-Benzyl (1,3-Dibenzyl)-4-(2-oxopropylidene)-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one
n ...
Ould Mohamed Sidya Mohamed Said +6 more
doaj +1 more source
Steric control of reactivity: formation of oximes, benzodiazepinone N-oxides and isoxazoloquinolinones [PDF]
Reaction of the alkenyl carbonyl compounds 1 with hydroxylamine can lead to the formation of the oximes 2, the benzodiazepinone N-oxides 3 or the isoxazoloquinolinones 5. The product(s) of reaction are shown to depend on the electronic nature of the terminal olefinic substituent R-3 and the space filling capacity of the substituents R-1, R-2 and R-4 ...
Heaney, Frances +3 more
openaire +3 more sources

