16287-28-8Relevant articles and documents
Synthesis of Benzodiazepines Through Ring Opening/Ring Closure of Benzimidazole Salts
Tao, Sheng,Bu, Qingqing,Shi, Qianqian,Wei, Donghui,Dai, Bin,Liu, Ning
supporting information, p. 3252 - 3258 (2020/03/04)
Pyrido-benzodiazepine derivatives are undoubtedly one of the most important structural motifs in the marketed drugs and the drug candidates. Commonly synthetic methods for construction of the benzodiazepine ring derivatives are based on the condensation reactions of two highly functionalized synthons. The development of synthesis for these compounds, however, is hampered by the regioselectivity and atom economy. In this work, a one-step synthesis of pyrido-benzodiazepine backbones and its analogues is achieved through continuous ring-opening hydrolysis of benzimidazole salts and intramolecular C?H bond activation. The reaction mechanism is explored by control experiments and density functional theory (DFT) calculations.
Palladium-mediated approach to dibenzo[b,e][1,4]diazepines and benzopyrido-analogues. An efficient synthesis of tarpane
Beccalli, Egle M.,Broggini, Gianluigi,Paladino, Giuseppe,Zoni, Caterina
, p. 61 - 68 (2007/10/03)
An original synthetic route toward dibenzo[b,e][1,4]diazepin-11-ones and analogues pyridobenzodiazepinones has been developed. The method relies upon an intramolecular amination process between an (hetero)aryl halide and the appropriate aniline moiety. Graphical Abstract.