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1-吡咯啉衍生物的合成——末端炔烃与 2-氮杂烯丙基的环化反应。

Synthesis of 1-pyrroline derivatives cyclization of terminal alkynes with 2-azaallyls.

机构信息

Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education, Yunnan Provincial Center for Research & Development of Natural Products, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, P. R. China.

出版信息

Org Biomol Chem. 2022 Apr 6;20(14):2843-2851. doi: 10.1039/d2ob00102k.

Abstract

An efficient transition-metal-free cyclization reaction to prepare 1-pyrroline derivatives bearing various functional groups is described. In this method, a simple combination of a base and a solvent allows the cyclization reaction of terminal alkynes and 2-azaallyls to be carried out efficiently under mild and metal-free conditions. This cyclization reaction will provide an efficient method for the synthesis of medicinally relevant polysubstituted and multifunctionalized pyrrolines.

摘要

描述了一种高效的无过渡金属环化反应,用于制备带有各种官能团的 1-吡咯啉衍生物。在该方法中,碱和溶剂的简单组合可以使末端炔烃和 2-氮杂烯丙基在温和无金属条件下有效地进行环化反应。该环化反应将为合成具有药用相关性的多取代和多功能化吡咯啉提供一种有效的方法。

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