László Poszávácz, T. Nagy, Katalin Kátai-Fadgyas
Jan 3, 2023
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Journal
Synthesis
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 apply explosive diazo reagents, moreover it is simple and safe, thereby suitable for scale-up.