16287-31-3Relevant academic research and scientific papers
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.
Benzodiazepine compounds and preparation method thereof
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Paragraph 0107-0112, (2020/03/05)
The invention belongs to the technical field of biological medicines, and particularly relates to benzodiazepine compounds and a preparation method thereof. A series of the benzodiazepine compounds provided by the invention are novel in structure, have certain drug potential, and have positive significance when applied to development of novel drugs. According to the invention, an N-heterocyclic bridged benzimidazolium salt is used as a raw material, inherent water in an organic solvent is utilized, and a ring opening-ring expanding reaction is conducted under the action of a catalyst so as toprepare the benzodiazepine compounds with an N-heterocyclic bridged seven-membered ring structure. The method provided by the invention has the advantages of mild conditions, no need for treatment ofthe solvent, simple steps, good regioselectivity and high atom economy.
