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

被引：0

作者：

Nassar, Youssef ^{[1
,2
]}

Rodier, Fabien ^{[3
,4
]}

Bigot, Antony ^{[5
]}

Cruciani, Paul ^{[2
,3
]}

Ferey, Vincent ^{[2
,6
]}

Daumas, Marc ^{[6
]}

Cossy, Janine ^{[1
]}

机构：

[1] ESPCI Paris, F-75005 Paris, France

[2] Sanofi M&S MSAT, Site Aramon, Route Avignon, F-30390 Aramon, France

[3] Sanofi, F-04200 Sisteron, France

[4] EUROAPI, F-04200 Sisteron, Provence Alpes, France

[5] Sanofi R&D, F-94400 Vitry Sur Seine, France

[6] Sanofi R&D, F-34080 Montpellier, France

来源：

ORGANIC LETTERS | 2025年 / 27卷 / 11期

关键词：

BREAST-CANCER;

D O I：

10.1021/acs.orglett.5c00772

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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)

引用

页码：2806 / 2810

页数：5

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