Allylic Acetal as 3C Synthon in Rh(III)-Catalyzed Divergent C–H Activation/[4 + 3] Annulation: Easy Access to Benzodiazepines

IF 5 1区化学 Q1 CHEMISTRY, ORGANIC

Organic Letters Pub Date : 2025-04-02 DOI:10.1021/acs.orglett.4c0439610.1021/acs.orglett.4c04396

Mingming Hu, Chao Pi*, Yangjie Wu and Xiuling Cui*,

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.

Abstract Image

查看原文本刊更多论文

丙烯醛缩醛在Rh（III）催化的C-H活化/[4 + 3]环合中的3C合成：苯二氮卓类药物的易得性

通过 Rh(III) 催化 C-H 活化/[4 + 3]环化容易获得的 1-芳基吡唑烷酮与烯丙基乙缩醛，开发了一种苯并二氮杂卓的简易合成方法。在这一转化过程中，烯丙基缩醛被用作新型 3C 合成物。在温和的反应条件下，以高效率和化学选择性生成了苯并二氮杂卓。高原子经济性和易于获得的底物揭示了其潜在的应用价值。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Organic Letters 化学-有机化学

CiteScore

9.30

自引率

11.50%

发文量

1607

审稿时长

1.5 months

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.