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- Title
Synthesis of Benzodiazepines Through Ring Opening/Ring Closure of Benzimidazole Salts.
- Authors
Tao, Sheng; Bu, Qingqing; Shi, Qianqian; Wei, Donghui; Dai, Bin; Liu, Ning
- Abstract
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.
- Subjects
BENZODIAZEPINES; DENSITY functional theory; CONDENSATION reactions; SALTS
- Publication
Chemistry - A European Journal, 2020, Vol 26, Issue 15, p3252
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201905828