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室温下通过 Rh(III)催化 C-H 活化和分子内级联环化合成高度稠合的吡喃并[2,3-]吡啶。

Synthesis of Highly Fused Pyrano[2,3-]pyridines via Rh(III)-Catalyzed C-H Activation and Intramolecular Cascade Annulation under Room Temperature.

机构信息

State Key Laboratory of Drug Research and CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China.

University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing 100049, China.

出版信息

J Org Chem. 2020 May 15;85(10):6281-6294. doi: 10.1021/acs.joc.9b03102. Epub 2020 Feb 25.

Abstract

A facile access to the polycyclic-fused pyrano[2,3-]pyridines has been established under room temperature via Rh(III)-catalyzed C-H bond activation and intramolecular cascade annulation. This strategy features high efficiency, unique versatility, and generality and it can occur under mild conditions in good to excellent yields. More importantly, this strategy can be extended to the late-stage functionalization of drugs possessing the CN group.

摘要

一种简便的方法,即在室温条件下,通过 Rh(III)-催化的 C-H 键活化和分子内级联环化,建立了多环稠合的吡喃并[2,3-]吡啶。该策略具有高效、独特的多功能性和通用性,并且可以在温和条件下以良好到优秀的收率进行。更重要的是,该策略可以扩展到具有 CN 基团的药物的后期功能化。

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