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Synthetic aspects of 1,4-and 1,5-benzodiazepines using o-phenylenediamine: a study of past quinquennial

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RSC ADVANCES
卷 13, 期 6, 页码 3694-3714

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ROYAL SOC CHEMISTRY
DOI: 10.1039/d2ra06045k

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Benzodiazepines are important compounds in the pharmaceutical industry, particularly 1,4- and 1,5-benzodiazepines which have various biological activities such as anticonvulsion, anti-anxiety, sedation, and hypnotics. Researchers have developed valuable and significant synthetic approaches for these moieties. This review article focuses on the systematic synthesis of 1,4- and 1,5-benzodiazepines using o-phenylenediamine as a precursor over the past five years (2018-2022), providing helpful insights for scientists and researchers seeking novel and efficient methods for their synthesis.
Benzodiazepines, seven-membered heterocyclic compounds having two nitrogen atoms at different positions, are ruling scaffolds in the area of pharmaceutical industry. They act as cardinal moieties in organic synthesis as well as in medicinal chemistry. Among the different benzodiazepines, 1,4- and 1,5-benzodiazepines play a far-reaching role in the field of biological activities such as anticonvulsion, anti-anxiety, sedation, and hypnotics. In the past few decades, researchers have conducted a lot of work on these moieties and developed broad, valuable, and significant approaches for their synthesis. In this review article, we recapitulate the systematic synthetic strategies of 1,4- and 1,5-benzodiazepines using o-phenylenediamine as a precursor over the past five years (2018-2022). This article will be helpful for scientists and researchers to examine and explore novel and efficient methods for the synthesis of these biologically active moieties.

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