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Synthesis 2023; 55(13): 2061-2069
DOI: 10.1055/a-2016-4337
DOI: 10.1055/a-2016-4337
paper
New, Scalable Process for the Preparation of 5-Acetyl-1H-pyrazole-3-carboxylic Acid, a Key Intermediate of Darolutamide
Dedicated to the memory of late Professor Ferenc Fülöp (1952–2021)
Abstract
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 employ explosive diazo reagents, moreover it is simple and safe, thereby suitable for scale-up.
Keywords
ester hydrolysis - regioselectivity - drug substance - key intermediate - safety - scalabilitySupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/a-2016-4337.
- Supporting Information
Publikationsverlauf
Eingereicht: 03. Januar 2023
Angenommen nach Revision: 19. Januar 2023
Accepted Manuscript online:
19. Januar 2023
Artikel online veröffentlicht:
14. März 2023
© 2023. Thieme. All rights reserved
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