Darolutamide关键中间体5-乙酰-1 H -吡唑-3-羧酸的可扩展制备新工艺

IF 2.2 4区化学 Q2 CHEMISTRY, ORGANIC Synthesis-Stuttgart Pub Date : 2023-01-03 DOI:10.1055/a-2016-4337

László Poszávácz, T. Nagy, Katalin Kátai-Fadgyas, Balázs Volk

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引用次数: 0

摘要

介绍了以吡唑-3,5-二羧酸二乙酯为原料合成达鲁他胺关键中间体- 5-乙酰基- 1h -吡唑-3-羧酸的新工艺。与文献中已知的合成路线相反，该方法不使用爆炸性重氮试剂，而且简单安全，适合规模化生产。

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New, Scalable Process for the Preparation of 5-Acetyl-1 H -pyrazole-3-carboxylic Acid, a Key Intermediate of Darolutamide

A new, efficient process for the synthesis of 5-acetyl-1H-pyrazole-3-carboxylic acid, a versatile building block and the key intermediate of darolutamide, using diethyl pyrazole-3,5-dicarboxylate as the starting material is described. Contrary to the synthetic routes known from the literature, this procedure does not apply explosive diazo reagents, moreover it is simple and safe, thereby suitable for scale-up.

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来源期刊

Synthesis-Stuttgart 化学-有机化学

CiteScore

4.50

自引率

7.70%

发文量

435

审稿时长

1 months

期刊介绍： SYNTHESIS is an international full-paper journal devoted to the advancement of the science of chemical synthesis. It covers all fields of organic chemistry involving synthesis, including catalysis, organometallic, medicinal, biological, and photochemistry, but also related disciplines. SYNTHESIS provides dependable research results with detailed and reliable experimental procedures and full characterization of all important new products as well as scientific primary data.