One-pot efficient pseudo-five-components synthesis of 4,4′-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ols) at room temperature assisted by K2CO3 (original) (raw)
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European Journal of Medicinal Chemistry, 2009
Substituted oxy/thio acetic acid ethyl esters LiHMDS Acid chloride Hydrazine hydrate 4-Oxy/thio substituted-1H-pyrazol-5(4H)ones Biological activity a b s t r a c t a-Oxy/thio substituted-b-keto esters were synthesized through an efficient cross-Claisen condensation of aryl oxy/thio acetic acid ethyl esters with acid chlorides, then it is converted in situ into 4-oxy/thio substituted-1H-pyrazol-5(4H)-ones by the addition of hydrazine or hydrazine derivatives and screened for their antibacterial, antifungal activities.
Simple and efficient one-pot synthesis of N-phenyl-3,5-difunctionalized pyrazoles
Tetrahedron, 2011
A facile one-pot synthesis of N-phenyl-3,5-difunctionalized pyrazoles is described. The dialkyl 2-[(Z)phenylhydrazono]succinate intermediate, which is prepared in situ from the mixture of phenylhydrazine and dialkyl acetylenedicarboxylate reacts with aroyl chloride or fumaryl chloride to afford the title compounds. Different types of compounds containing COCl functional group were used to investigate the scope and limitation of the reaction. Two eCO 2 R and eO 2 C groups at 3-and 5-position are potentially capable to convert to other functional groups. The reaction conditions are relatively mild and the yields are good.
An Efficient One Pot Synthesis and Biological Screening of Some Pyrazole Based Heterocycles
Chemical Science, 2020
Present work deals with the preparation of some Pyrazole derivative salts which was prepared by using different kinds of aldehydes and hydrazine derivatives by using alkoxide as a base and using the 1,3-dicarbonyl compound like ethyl acetoacetate at room temperature. The reaction mixture was stirred on magnetic stirrer for about 10 to 20 minutes till colour change is observed and then product is separated by using organic solvent. The product obtained was converted to sodium salt of Pyrazole derivative by base hydrolysis. The entire synthesized compound was tested for their antibacterial activity against the Gram-positive and Gram-negative strains of bacteria. The investigation of antibacterial screening data revealed that most of the tested compounds showed moderate to good antibacterial activity.
Journal of Pharmaceutical Research International, 2021
Pyrazoles are reported to be well known pharmacophores. This has motivated the synthesize some of the pyrazole derivatives by using hydrazine hydrate as well as adding benzimidazole in pyrazoles. A series of (4Z)-2-(1H-benzimidazol-2-ylmethyl)-4-arylidene-5-methyl-2,4-dihydro-3H-pyrazol-3-ones (IIIa3 to IIIe3) was synthesized by conventional method by refluxing compounds (IIIa2-IIIe2) with O-Phenylene diamine in absolute ethanol. A series of compounds (IIIa2-IIIe2) was prepared by reacting compounds (IIIa1-IIIe1) with chloroacetic acid. A series of (4E)-4-arylidene-5-methyl-2,4–dihydro-3H-pyrazol-3-ones (IIIa1-IIIe1) was prepared by the reaction between 5-methyl-2,4-dihydro- 3H-pyrazol-3-one (II) and different aldehydes in presence of Sodium acetate. All of the compounds were synthesised with high yields (58-80%) and identified using IR, 1H NMR spectrum data, as well as C, H, and N elemental analyses. At varying MIC values, all of the produced compounds showed antibacterial and a...