一种定义良好的n -杂环钯（NHC）催化剂催化的双硼酸酯的Suzuki-Miyaura偶联

IF 3.5 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-06-03 DOI:10.1021/acsmedchemlett.5c0020610.1021/acsmedchemlett.5c00206

Aleksei A. Logvinov, Geert Rombouts, Matthieu Jouffroy* and Steven P. Nolan*,

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引用次数: 0

摘要

我们报道了一种多用途的合成方法，将杂芳基氯化物和溴化物与具有药用价值的杂芳基蒎烯硼酯偶联，在低催化剂负载下，在一个定义良好的钯- nhc催化剂上，在短反应时间内提供高分离收率和纯度的产品。该方法对5元杂环和6元杂环均具有广泛的适用性。

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Suzuki–Miyaura Coupling of Pinacolboronic Esters Catalyzed by a Well-Defined Palladium N-Heterocyclic Carbene (NHC) Catalyst

We report a versatile synthetic method for coupling heteroaryl chlorides and bromides with (hetero)aryl pinacolboronic esters of pharmaceutical interest at low catalyst loading of a well-defined palladium-NHC catalyst providing products in good to high isolated yield and purity in short reaction time. The method displays remarkably broad applicability with both 5- and 6-membered heterocycles.

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来源期刊

ACS Medicinal Chemistry Letters CHEMISTRY, MEDICINAL-

CiteScore

7.30

自引率

2.40%

发文量

328

审稿时长

1 months

期刊介绍： ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to: Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics) Biological characterization of new molecular entities in the context of drug discovery Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc. Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic Mechanistic drug metabolism and regulation of metabolic enzyme gene expression Chemistry patents relevant to the medicinal chemistry field.