20629-92-9

Upstream product

• 141-97-9 ethyl acetoacetate 
• 1073-69-4 N-4-chlorophenylhydrazine 
• 105-45-3 acetoacetic acid methyl ester 

Downstream Products

• 99853-56-2 2-(4’-chlorophenyl)-1,5-dimethyl-1,2-dihydro-3H-pyrazol-3-one 
• 77509-93-4 5-chloro-1-(4-chlorophenyl)-3-methyl-1H-pyrazole-4-carbaldehyde 
• 1067647-67-9 1-(4-chlorophenyl)-2,5-dihydro-α-hydroxy-3-methyl-5-oxo-α-trifluoromethyl-1H-pyrazole-4-acetic acid methyl ester 

Relevant academic research and scientific papers

Containing substituted 1, 3, 4-thiadiazole sulfide pyrazole amide and pyrazole imine derivatives and preparation method and application

The invention discloses pyrazole amide and pyrazole imine derivatives containing substituted 1, 3, 4-thiadiazole thioether as well as a preparation method and an application of the derivatives. The compounds have the structures as shown in formulae (I) and (II). The preparation method comprises the following steps: by taking substituted hydrazine as an initial raw material, carrying out closed loop, chlorine formylation, oxidation and chloro reaction to obtain pyrazole acyl chloride; carrying out a reaction on 2-amino-5-mercapto-1, 3, 4-thiadiazole and substituted benzyl chloride to obtain 2-amino-5-substituted 1, 3, 4-thiadiazole thioether; and then, carrying out a substitution reaction on 2-amino-5-substituted 1, 3, 4-thiadiazole thioether and substituted pyrazole acyl chloride to obtain the pyrazole amide compound (I) containing substituted 1, 3, 4-thiadiazole thioether; by taking substituted hydrazine as an initial raw material, carrying out closed loop and chlorine formylation to obtain pyrazole aldehyde; carrying out an additive elimination reaction on pyrazole aldehyde and 2-amino-5-mercapto-1, 3, 4-thiadiazole under a backflow condition of anhydrous ethanol to obtain 2-substituted pyrazole imidogen-5-mercapto-1, 3, 4-thiadiazole; and then carrying out a reaction on 2-substituted pyrazole imidogen-5-mercapto-1, 3, 4-thiadiazole and substituted benzyl chloride to generate the pyrazole imine compound (II) containing substituted 1, 3, 4-thiadiazole thioether. The compounds disclosed by the invention have a good inhibiting effect on tobacco mosaic virus and can be used for preparing anti-plant virus drugs.

Cobalt doped ZnS nanoparticles as a recyclable catalyst for solvent-free synthesis of heterocyclic privileged medicinal scaffolds under infrared irradiation

This paper reports preparation and characterization of cobalt doped ZnS NPs and their catalytic application in the synthesis of heterocyclic privileged medicinal scaffolds involving pyrazolones (with excellent regioselectivity) and 1,3-oxathiolan-5-one frameworks under infrared irradiation. Nanoparticles have been prepared at room temperature by a wet chemical method. The heterogeneous catalysts were fully characterized by XRD, TEM, EDAX, ICP-AES and UV/Vis. Under infrared radiation (IR), the catalytic activity of Co doped ZnS NPs was about 40-fold higher under IR as compared to the conventional method. Nanocatalyst plays a dual role of catalyst as well as susceptor, and enhances the overall capacity to absorb IR in the reaction mixture. Doping by Co promotes the activity and selectivity of ZnS NPs as indicated by their high TOF value, providing the products with good to excellent yields. The surface acidity of NPs was measured by FTIR spectra of chemisorbed pyridine. The present method does not involve any hazardous organic solvent or catalyst. The introduction of nanocatalyst in an IR system offers promising features for the reaction response such as the shorter reaction time, simple work-up procedure, and purification of products by non-chromatographic methods. The catalyst was reused up to four runs without an appreciable loss of catalytic activity.

Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists

The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.