Structure of 1,5-benzodiazepinones in the solid state and in solution: Effect of the fluorination in the six-membered ring [PDF]
Beilstein Journal of Organic Chemistry, 2013 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 +2 more
exaly +4 more sources
Regioselective Halogenation of 1,4-Benzodiazepinones via CH Activation [PDF]
Scientific Reports, 2015 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 ...
Jean-Christophe Cintrat
exaly +7 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]
Molecules, 2022 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 +3 more sources
Copper-promoted synthesis of 1,4-benzodiazepinones via alkene diamination [PDF]
Tetrahedron Letters, 2015 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.
Shuklendu D Karyakarte, Sherry R Chemler
exaly +5 more sources
SYNTHESIS OF NEW FUSED BENZOPYRANO-BENZODIAZEPINONES
Heterocyclic Communications, 2002 Zine Mighri
exaly +3 more sources
A novel Pd-catalysed sequential carbonylation/cyclization approach toward bis-N-heterocycles: rationalization by electronic structure calculations [PDF]
Royal Society Open Science, 2018 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
Benzodiazepinone Derivatives as CRTH2 Antagonists. [PDF]
ACS Med Chem Lett, 2011 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- and Silver-Catalyzed Reactions of Active Methylene Isocyanides: Facile Access to Highly Substituted Five- and Six-Membered Heterocycles. [PDF]
ChemistryThis 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
Synthesis of tetrazolo-fused benzodiazepines and benzodiazepinones by a two-step protocol using an Ugi-azide reaction for initial diversity generation [PDF]
Tetrahedron, 2012 Steven Gunawan +2 more
exaly +2 more sources
Synthesis of Indole‐Fused 1,4‐Diazepinones via Photoredox‐Catalyzed Cascade Cyclization Reaction
Advanced Synthesis &Catalysis, Volume 365, Issue 22, Page 3958-3966, November 21, 2023., 2023 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