Synthesis of Multi-Substituted β-Carbolin-1-ones via Iridium-Catalyzed Intramolecular C─H/N─H Amination of 3-Amino-2-pyridones

IF 2.7 4区化学 Q1 CHEMISTRY, ORGANIC

Asian Journal of Organic Chemistry Pub Date : 2025-07-17 DOI:10.1002/ajoc.202500425

Honoka Mori, Maho Morimura, Ayana Okada, Hiroyoshi Masuda, Prof. Dr. Iwao Hachiya

引用次数: 0

Abstract

A method for the synthesis of multi-substituted β-carbolin-1-ones is developed, utilizing iridium-catalyzed intramolecular C─H/N─H amination of 3-amino-2-pyridones synthesized via the conjugate addition of diethyl 2-aminomalonate to alkynyl imines. This synthetic strategy was successfully applied to the formal synthesis of an antidiabetic agent.

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铱催化3-氨基-2-吡啶酮分子内C─H/N─H胺化合成多取代β-碳-1-酮

利用铱催化的2-氨基丙二酸二乙酯与炔基亚胺共轭加成的3-氨基-2-吡啶酮分子内C─H/N─H胺化反应，提出了一种合成多取代β-羰基-1-酮的方法。该合成策略已成功应用于抗糖尿病药物的正式合成。

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来源期刊

Asian Journal of Organic Chemistry CHEMISTRY, ORGANIC-

CiteScore

4.70

自引率

3.70%

发文量

372

期刊介绍： Organic chemistry is the fundamental science that stands at the heart of chemistry, biology, and materials science. Research in these areas is vigorous and truly international, with three major regions making almost equal contributions: America, Europe and Asia. Asia now has its own top international organic chemistry journal—the Asian Journal of Organic Chemistry (AsianJOC) The AsianJOC is designed to be a top-ranked international research journal and publishes primary research as well as critical secondary information from authors across the world. The journal covers organic chemistry in its entirety. Authors and readers come from academia, the chemical industry, and government laboratories.