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铜(I)催化的β,γ-不饱和腙的加氧氨化反应:二氢吡唑的合成。

Copper(I)-Catalyzed Oxyamination of β,γ-Unsaturated Hydrazones: Synthesis of Dihydropyrazoles.

机构信息

Key Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital , Guangzhou Medical University , Guangzhou , Guangdong 511436 , China.

Department of Pharmaceutical Production Center , The First Affiliated Hospital of Hunan University of Chinese Medicine , Changsha , Hunan 410007 , China.

出版信息

Org Lett. 2019 Oct 4;21(19):7787-7790. doi: 10.1021/acs.orglett.9b02733. Epub 2019 Sep 20.

DOI:10.1021/acs.orglett.9b02733
PMID:31539265
Abstract

An efficient aerobic copper(I)-catalyzed oxyamination of β,γ-unsaturated hydrazones has been developed. The methodology provides effective access to dihydropyrazole derivatives in a one-pot process utilizing dioxygen as a sustainable sacrificial oxidant. Mechanistic studies have been performed and are suggestive of an aerobic manifold via single electron transfer.

摘要

一种高效的有氧铜(I)催化β,γ-不饱和腙的氧胺化反应已经被开发出来。该方法利用氧气作为可持续的牺牲氧化剂,在一锅反应中提供了有效合成二氢吡唑衍生物的途径。已经进行了机理研究,表明该反应是通过单电子转移的有氧途径进行的。

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