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385381-91-9

5-THIOPHEN-2-YL-2,4-DIHYDRO-PYRAZOL-3-ONE synthesis

2synthesis methods
-

Yield:385381-91-9 43%

Reaction Conditions:

with hydrazine hydrate in ethanol; for 3 h;Reflux;

Steps:

General Method for the Preparation of Pyrazolones

[0106] Hydrazine monohydrate 64% (2.25 ml, 29.4 mmol, 1.05 equiv.) was added dropwise to a solution of the β-ketoester in absolute ethanol (28 mmol, c = 0.19 M). The resulting orange solution was stirred under reflux for 3 hours. Conversion was checked by NMR, (few drops of the reaction mixture were dried under a stream of air and dissolved in CDCI3) and upon disappearance of the starting material, the solvent was evaporated under reduced pressure and the resulting solid was triturated with acetone or ethanol.

References:

WO2018/183587,2018,A1 Location in patent:Paragraph 0106-0107