Pyridine Synthesis via [3 + 2 + 1] Oxidative Cyclization of Enamines, Ethyl Tertiary Amines, and Alcohols: Copper-Catalyzed Cascade Multicomponent Poly C(sp <sup>3</sup> )–H Functionalization

A copper-catalyzed [3 + 2 + 1] oxidative cyclization to access functionalized pyridines was descripted. Employing ethyl tertiary amine as a C2 source, alcohol as a C1 source, and easily handled enamines, one new C-N bond and two new C-C bonds are sequentially constructed by the effective functionalization of multiple C(sp<sup>3</sup>)-H bonds. Besides the readily available raw materials, mild reaction conditions, broad substrate scope, and effective bond-forming strategy, the present approach offers a viable strategy for preparing functionalized pyridines in future organic synthesis.

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Publication Details

Journal
Organic Letters
Published
2026-02-13
DOI
https://doi.org/10.1021/acs.orglett.6c00130
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
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article

Pyridine Synthesis via [3 + 2 + 1] Oxidative Cyclization of Enamines, Ethyl Tertiary Amines, and Alcohols: Copper-Catalyzed Cascade Multicomponent Poly C(sp 3 )–H Functionalization

Zijing Bai, Peng Gao, Jingzhi Cheng, Binghan Du et al.
Organic Letters
Catalytic C–H Functionalization Methods
article

Pyridine Synthesis via [3 + 2 + 1] Oxidative Cyclization of Enamines, Ethyl Tertiary Amines, and Alcohols: Copper-Catalyzed Cascade Multicomponent Poly C(sp 3 )–H Functionalization

Zijing Bai, Peng Gao, Jingzhi Cheng, Binghan Du, Yutong He, Wei Shi, Chengli Deng, Ruimin He
article en

Abstract

A copper-catalyzed [3 + 2 + 1] oxidative cyclization to access functionalized pyridines was descripted. Employing ethyl tertiary amine as a C2 source, alcohol as a C1 source, and easily handled enamines, one new C-N bond and two new C-C bonds are sequentially constructed by the effective functionalization of multiple C(sp<sup>3</sup>)-H bonds. Besides the readily available raw materials, mild reaction conditions, broad substrate scope, and effective bond-forming strategy, the present approach offers a viable strategy for preparing functionalized pyridines in future organic synthesis.

Organic LettersVol. 28(8)
Baoji University of Arts and Sciences (CN), Institute of Organic Chemistry with Centre of Phytochemistry (BG), Yuxi Normal University (CN)
Openalex Percentile: Top 54%
Catalytic C–H Functionalization Methods
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