Highly efficient CuI nanoparticles catalyzed one-pot synthesis of some benzo[b][1,5]diazepine derivatives via multi-component condensation of aromatic diamines, Meldrum's acid and isocyanides. The present approach creates a variety of benzo[b][1,5]diazepines as pharmaceutical and biologically active heterocyclic compounds in excellent yields and short reaction times. The salient features of the...

The asymmetric unit of the title compound, C(20)H(17)N(3), contains two crystallographically independent mol-ecules (A and B). In mol-ecule A, the two benzene rings form dihedral angles of 74.12 (7) and 7.83 (7)° with the pyridine ring, while in mol-ecule B these angles are 77.48 (7) and 21.50 (7)°. The seven-membered heterocyclic ring adopts a boat conformation in both mol-ecules. In the cryst...

Three novel chelators based on the 6-amino-6-methylperhydro-1,4-diazepine scaffold and possessing three pendant N-acetic or N-α-methylacetic acid have been synthesised. The ligands contain six donor atoms for complexation of Mn(II) ions and thus potentially leave an additional site for coordination of a water molecule. The protonation constants of the ligands and the stability constants of thei...

was positive but the rest of tested benzodiazepines were negative. Previous reports2 suggest that there is no cross-reactivity among benzodiazepines. Diazepam is the most similar benzodiazepine to tetrazepam, the only difference between them is the presence at position 5 on the diazepine ring of phenyl in diazepam and clohexen in tetrazepam, and this cyclohexene conformation could explain tetra...

In the reaction of 7-chloro-1,5-benzodiazepine-2,4-dione with N,N-dimethyl-formamide/dimethyl-acetal, the diazepine seven-membered ring undergoes a contraction to form the five-membered ring. The reaction yields two isomers the title compound, C(13)H(14)ClN(3)O(2); the major component has the chlorine-atom substituent in the 5-position of the benzimidazolone ring and the minor component has the...

Imidazo[1,5-a][1,4]benzodiazepines are well documented to exhibit potent activity at GABAA/Bz receptors. This series belongs to one of the very few chemical families, which have been extensively investigated for GABAA/Bz receptor mediated activity.1,2 Flumazenil (Ro 15-1788), an imidazo[1,5-a][1,4]benzodiazepine, was earlier shown to bind to central GABAA receptors with little or no intrinsic a...

Synthetic approaches are reported to polydentate ligands based on 6-phenyl-6-amino-perhydro-1,4-diazepine. The synthetic route devised averts ring-opening reactions, allowing the exocyclic N-substituent to be introduced separately and involves a nitro-Mannich condensation, prior to chemoselective RANEY® nickel reduction. Comparison of the solid-state structures of four synthetic intermediates r...

We describe new synthetic routes developed toward a range of substituted analogues of bromo and extra-terminal (BET) bromodomain inhibitors I-BET762/JQ1 based on the triazolo-benzodiazepine scaffold. These new routes allow for the derivatization of the methoxyphenyl and chlorophenyl rings, in addition to the diazepine ternary center and the side chain methylene moiety. Substitution at the level...