Synthetic Transformations of Higher Terpenoids. 45^#. Regioselective Synthesis of 5-Labdanoid-Substituted Pyrazoles and Assessment of Their Analgesic Activity

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发表日期：

2024年7月1日

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M. E. Mironov,
A. I. Poltanovich,
V. I. Krasnov,
T. V. Rybalova,
S. A. Borisov,
T. G. Tolstikova,
E. E. Shults

摘要

A method for targeted structural modification of the methyl ester of phlomisoic acid was developed by introduction of an additional C-16 ketopyrazole moiety via cyclocondensation of diterpenoid alkyne-1,2- diones with arylhydrazines. The conditions for regioselective formation of labdanoid 1,3-diarylpyrazol-5- ylmethanones were found. The possibility of a sequential four-component reaction in a single pot was demonstrated. Significant analgesic activity of labdanoid-substituted diarylpyrazoles in thermal and chemical irritation models was established.

Synthetic Transformations of Higher Terpenoids. 45#. Regioselective Synthesis of 5-Labdanoid-Substituted Pyrazoles and Assessment of Their Analgesic Activity

摘要

Synthetic Transformations of Higher Terpenoids. 45^#. Regioselective Synthesis of 5-Labdanoid-Substituted Pyrazoles and Assessment of Their Analgesic Activity