{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,11]],"date-time":"2026-08-11T23:38:41Z","timestamp":1786491521745,"version":"build-2736575974"},"reference-count":98,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2026,6,8]],"date-time":"2026-06-08T00:00:00Z","timestamp":1780876800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100004242","name":"Princess Nourah bint Abdulrahman University","doi-asserted-by":"publisher","award":["RAP-2026-71"],"award-info":[{"award-number":["RAP-2026-71"]}],"id":[{"id":"10.13039\/501100004242","id-type":"DOI","asserted-by":"publisher"}]},{"award":["RAP-2026-71"],"award-info":[{"award-number":["RAP-2026-71"]}],"id":[{"id":"https:\/\/ror.org\/05b0cyh02","id-type":"ROR","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>1,5-Benzodiazepin-2-one is a significant class of heterocyclic compounds that have attracted considerable attention due to these versatile scaffolds and their multifunctional properties. Owing to the presence of a fused benzene\u2013diazepine core, these compounds display rich chemical reactivity and various physicochemical characteristics, making them valuable structures in both fundamental and applied research. This review provides a comprehensive and critical overview of the advances reported to date on 1,5-benzodiazepin-2-ones, with particular emphasis on their diverse synthetic methodologies, reaction mechanisms, and structure\u2013property relationships. Classical and modern synthetic approaches are discussed, including condensation reactions, multicomponent processes, catalytic and green chemistry approaches, as well as recent developments toward more sustainable and efficient protocols. The intrinsic reactivity of the 1,5-benzodiazepin-2-one framework enables access to structurally diverse derivatives. Furthermore, the review summarizes the broad range of applications of these heterocycles, especially in medicinal chemistry, where they have demonstrated significant biological activities, as well as in corrosion inhibition and photoluminescent materials. Finally, current challenges, limitations, and future perspectives are outlined to provide guidance for further research and development of 1,5-benzodiazepin-2-one-based systems.<\/jats:p>","DOI":"10.3390\/molecules31122004","type":"journal-article","created":{"date-parts":[[2026,6,8]],"date-time":"2026-06-08T16:25:16Z","timestamp":1780935916000},"page":"2004","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["The 1,5-Benzodiazepin-2-Ones: A Review on Synthetic Strategies, Reactivity and Functional Applications"],"prefix":"10.3390","volume":"31","author":[{"ORCID":"https:\/\/orcid.org\/0009-0001-7361-0956","authenticated-orcid":false,"given":"Hasan","family":"Mtiraou","sequence":"first","affiliation":[{"name":"Laboratory of Heterocyclic Chemistry Natural Products and Reactivity\/CHPNR, Department of Chemistry, Faculty of Science of Monastir, University of Monastir, Monastir 5000, Tunisia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ameni","family":"Ghabi","sequence":"additional","affiliation":[{"name":"Laboratory of Heterocyclic Chemistry Natural Products and Reactivity\/CHPNR, Department of Chemistry, Faculty of Science of Monastir, University of Monastir, Monastir 5000, Tunisia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hanan","family":"Al-Ghulikah","sequence":"additional","affiliation":[{"name":"Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7038-8018","authenticated-orcid":false,"given":"Mezna Saleh","family":"Altowyan","sequence":"additional","affiliation":[{"name":"Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2026,6,8]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"301","DOI":"10.2174\/0122133372300414240403035407","article-title":"Solvent-Free Synthesis of Bioactive Heterocycles","volume":"11","author":"Bajpai","year":"2024","journal-title":"Curr. 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