Facile Access to 1,5-Benzodiazepines via Amine-Promoted (4+3) Annulations of δ-Acetoxy Allenoates with o-Diaminobenzenes under Mild Conditions,Synlett

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Facile Access to 1,5-Benzodiazepines via Amine-Promoted (4+3) Annulations of δ-Acetoxy Allenoates with o-Diaminobenzenes under Mild Conditions
Synlett ( IF 1.7 ) Pub Date : 2018-03-23 , DOI: 10.1055/s-0037-1609347
Yi-Fan Wang ₁ , Cheng-Yu He ₂ , Longlei Hou ₁ , Ping Tian _{2,

3} , Guo-Qiang Lin _{2,

3} , Xiaofeng Tong ₁

Affiliation

An amine-promoted (4+3) annulation of δ-acetoxy allenoate with o-diaminobenzene is reported, providing a facile access to 1,5-benzodiazepine. This method features wide reaction scope, mild conditions, and readily available starting materials. The cascade reaction involves aza-Michael addition of o-diaminobenzene to allenoate, elimination of acetate group, and subsequent 1,6-aza-Michael addition.

中文翻译：

在温和条件下，通过胺促进 (4+3) δ-乙酰氧基苯甲酸酯与邻二氨基苯的环化，轻松获得 1,5-苯二氮卓类药物

据报道，胺促进 (4+3) δ-乙酰氧基烯丙酸酯与邻二氨基苯成环，提供了轻松获得 1,5-苯二氮卓的途径。该方法反应范围广，条件温和，原料易得。级联反应包括邻二氨基苯与烯丙酸酯的氮杂-迈克尔加成、乙酸酯基团的消除以及随后的 1,6-氮杂-迈克尔加成。

更新日期：2018-03-23

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