{"title":"Allylic Acetal as 3C Synthon in Rh(III)-Catalyzed Divergent C–H Activation/[4 + 3] Annulation: Easy Access to Benzodiazepines","authors":"Mingming Hu, Chao Pi, Yangjie Wu, Xiuling Cui","doi":"10.1021/acs.orglett.4c04396","DOIUrl":null,"url":null,"abstract":"A concise synthesis of benzodiazepines via Rh(III) catalyzed C–H activation/ [4 + 3] annulation of easily available 1-arylpyrazolidinones with allylic acetal has been developed. The allylic acetal was employed as a novel 3C synthon in this transformation. Benzodiazepines were built under mild reaction conditions with high efficiency and chemoselectivity. The high atom-economy and easily accessible substrates reveal potential application.","PeriodicalId":54,"journal":{"name":"Organic Letters","volume":"23 1","pages":""},"PeriodicalIF":5.0000,"publicationDate":"2025-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Organic Letters","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1021/acs.orglett.4c04396","RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
引用次数: 0
Abstract
A concise synthesis of benzodiazepines via Rh(III) catalyzed C–H activation/ [4 + 3] annulation of easily available 1-arylpyrazolidinones with allylic acetal has been developed. The allylic acetal was employed as a novel 3C synthon in this transformation. Benzodiazepines were built under mild reaction conditions with high efficiency and chemoselectivity. The high atom-economy and easily accessible substrates reveal potential application.
期刊介绍：
Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.
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