In this section, you can access to the latest technical information related to the FUTURE project topic.

Synthesis of Benzodiazepines Through Ring Opening/Ring Closure of Benzimidazole Salts

Taylor?made benzodiazepines: 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.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.

» Author: Sheng Tao, Qingqing Bu, Qianqian Shi, Donghui Wei, Bin Dai, Ning Liu

» Reference: doi:10.1002/chem.201905828

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