New, scalable process for the preparation of 5-acetyl-1H-pyrazole-3-carboxylic acid, a key intermediate of darolutamide
1
Directorate of Drug Substance Development, Egis Pharmaceuticals Plc, Budapest, Hungary
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Publication type: Journal Article
Publication date: 2023-01-19
scimago Q2
wos Q2
SJR: 0.559
CiteScore: 4.6
Impact factor: 2.3
ISSN: 00397881, 1437210X
Catalysis
Organic Chemistry
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.
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Poszávácz L. et al. New, scalable process for the preparation of 5-acetyl-1H-pyrazole-3-carboxylic acid, a key intermediate of darolutamide // Synthesis. 2023. Vol. 55. No. 13. pp. 2061-2069.
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Poszávácz L., Nagy T., Kátai Fadgyas K., Volk B. New, scalable process for the preparation of 5-acetyl-1H-pyrazole-3-carboxylic acid, a key intermediate of darolutamide // Synthesis. 2023. Vol. 55. No. 13. pp. 2061-2069.
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TY - JOUR
DO - 10.1055/a-2016-4337
UR - https://doi.org/10.1055/a-2016-4337
TI - New, scalable process for the preparation of 5-acetyl-1H-pyrazole-3-carboxylic acid, a key intermediate of darolutamide
T2 - Synthesis
AU - Poszávácz, László
AU - Nagy, Tamás
AU - Kátai Fadgyas, Katalin
AU - Volk, Balázs
PY - 2023
DA - 2023/01/19
PB - Georg Thieme Verlag KG
SP - 2061-2069
IS - 13
VL - 55
SN - 0039-7881
SN - 1437-210X
ER -
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BibTex (up to 50 authors)
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@article{2023_Poszávácz,
author = {László Poszávácz and Tamás Nagy and Katalin Kátai Fadgyas and Balázs Volk},
title = {New, scalable process for the preparation of 5-acetyl-1H-pyrazole-3-carboxylic acid, a key intermediate of darolutamide},
journal = {Synthesis},
year = {2023},
volume = {55},
publisher = {Georg Thieme Verlag KG},
month = {jan},
url = {https://doi.org/10.1055/a-2016-4337},
number = {13},
pages = {2061--2069},
doi = {10.1055/a-2016-4337}
}
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MLA
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Poszávácz, László, et al. “New, scalable process for the preparation of 5-acetyl-1H-pyrazole-3-carboxylic acid, a key intermediate of darolutamide.” Synthesis, vol. 55, no. 13, Jan. 2023, pp. 2061-2069. https://doi.org/10.1055/a-2016-4337.