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A Diastereoselective Route to Benzoannelated Bridged Sultams
Synthesis ( IF 2.2 ) Pub Date : 2021-06-17 , DOI: 10.1055/a-1531-2176
Victor V. Sokolov , Anastasiia A. Klochkova , Valentin A. Rassadin

A practical diastereoselective method for the synthesis of benzoannelated tri- and tetracyclic bridged sultams has been developed. The synthetic route employs widely available, substituted o-iodoanilines and is based on intramolecular Michael addition followed by cycloalkylation with α,ω-dihaloalkanes, or vice versa. The target compounds were isolated in good yields and the diastereoselectivity of the reaction could be easily controlled by the order of Michael addition and cycloalkylation steps.

中文翻译:

苯并退火桥接 Sultams 的非对映选择性途径

已开发出一种实用的非对映选择性方法,用于合成苯甲酰化的三环和四环桥连 sultam。合成路线采用广泛可用的取代邻碘苯胺,基于分子内迈克尔加成,然后与 α,ω-二卤代烷烃环烷基化,反之亦然。目标化合物以良好的收率分离,反应的非对映选择性可以通过迈克尔加成和环烷基化步骤的顺序轻松控制。
更新日期:2021-08-05
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