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 +3 more sources
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
Mannich-Type Condensation and Domino Quinazolinone-Amidine Rearrangement Affords Ring-Fused Mackinazolinones with Anti-Amoebic Activity. [PDF]
Abstract A three‐step synthesis of anti‐amoebic, ring‐fused mackinazolinones has been developed. A Mannich‐type reaction between quinazolin‐4‐ones and N‐Cbz propanal in the presence of AgOTf afforded quinazolinones (19–94% isolated yield) bearing a newly formed heterocycle with an alkylamine appendage that, upon N‐Cbz deprotection and basification ...
Lish MS +5 more
europepmc +2 more sources
Copper- and Silver-Catalyzed Reactions of Active Methylene Isocyanides: Facile Access to Highly Substituted Five- and Six-Membered Heterocycles. [PDF]
This review summarizes recent advances in copper‐ and silver‐catalyzed reactions of active methylene isocyanides for the synthesis of highly substituted five‐ and six‐membered heterocycles. Emphasis is placed on [3+n] cycloadditions, annulations, and asymmetric strategies, highlighting current limitations and future opportunities in heterocycle ...
George J, Oh K.
europepmc +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
Copper-promoted synthesis of 1,4-benzodiazepinones via alkene diamination. [PDF]
Karyakarte SD +6 more
europepmc +2 more sources
Regioselective Halogenation of 1,4-Benzodiazepinones via CH Activation. [PDF]
Abdelkafi H, Cintrat JC.
europepmc +2 more sources
Synthesis of Indole‐Fused 1,4‐Diazepinones via Photoredox‐Catalyzed Cascade Cyclization Reaction
Abstract A photoredox‐promoted approach for the synthesis of [1,4]diazepino[1,7‐a]indol‐6(7H)‐ones starting from N‐indolyl phenylacrylamides and aroyl chlorides as radical source is reported. This method, that involves a cascade radical addition on C−C double bond followed by intramolecular cyclization at indole C2‐position, affords two diastereomeric ...
Elisa Brambilla +6 more
wiley +1 more source
Anticancer and Antimicrobial Activity of Some New 2,3‐Dihydro‐1,5‐benzodiazepine Derivatives
A series of 2,3‐dihydro‐1,5‐benzodiazepine derivatives have been synthesized and characterized using IR, NMR, GC‐MS, single crystal XRD, and microanalysis. The results of their antibacterial activity against methicillin‐resistance Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Bacillus subtilis, Streptococcus mutans, Pseudomonas ...
Felix Odame +7 more
wiley +1 more source
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

