Amcenestrant （SAR439859）的合成：铜催化的交叉偶联反应可替代钯催化的Suzuki反应

IF 5 1区化学 Q1 CHEMISTRY, ORGANIC Organic Letters Pub Date : 2025-03-07 DOI:10.1021/acs.orglett.5c00772

Youssef Nassar, Fabien Rodier, Antony Bigot, Paul Cruciani, Vincent Ferey, Marc Daumas, Janine Cossy

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引用次数: 0

摘要

三氟化烯醇和芳基格氏试剂在铜催化剂下发生交叉偶联反应，接着是脱保护步骤、光信反应和皂化反应，从而合成Amcenestrant （SAR439859）。这种方法避免了昂贵和有毒的过渡金属，与传统方法一样有效，但在获取选择性雌激素受体降解剂（SERD）方面更便宜。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Synthesis of Amcenestrant (SAR439859): A Copper-Catalyzed Cross-Coupling Reaction as a Sustainable Alternative to Palladium-Catalyzed Suzuki Reaction

A cross-coupling reaction between an enol triflate and an aryl Grignard reagent using a copper catalyst, followed by a deprotection step, a Mitsunobu reaction, and a saponification, allowed for the synthesis of Amcenestrant (SAR439859). This approach, avoiding an expensive and toxic transition metal, is as efficient as the classical route but less expensive for accessing this selective estrogen-receptor degrader (SERD)

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来源期刊

Organic Letters 化学-有机化学

CiteScore

9.30

自引率

11.50%

发文量

1607

审稿时长

1.5 months

期刊介绍： Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.