63500-31-2

Upstream product

• 39833-49-3 1-phenyl-3-(4-nitrophenyl)-2-propyn-1-one 
• 60-34-4 methylhydrazine 
• 3672-66-0 1-(4-nitrophenyl)-3-phenylprop-2-yn-1-one 
• 1226790-03-9 C₉H₅Br₂NO₃ 
• 57-14-7 N,N-Dimethylhydrazine 
• 98-80-6 phenylboronic acid 
• 1627-14-1 N-methyl-N'-(4'-nitrobenzylidene)benzenesulfonohydrazide 
• 536-74-3 phenylacetylene 
• 1018817-75-8 1-methyl-3-(4-nitrophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole 
• 122-04-3 4-nitro-benzoyl chloride 
• 98-88-4 benzoyl chloride 
• 937-31-5 (4-Nitrophenyl)acetylene 
• 636-98-6 p-nitrobenzene iodide 

Relevant academic research and scientific papers

Preparation method for pyrazole

The invention relates to a preparation method for pyrazole, belonging to the field of organic chemistry. The preparation method disclosed in the invention realizes preparation of pyrazole through a cyclization reaction of N-alkylated phenylsulfonylhydrazone with terminal alkyne. The reaction has good function group tolerance and high yield and is applicable to a wide range of substrates.

Aluminum Chloride Mediated Reactions of N-Alkylated Tosylhydrazones and Terminal Alkynes: A Regioselective Approach to 1,3,5-Trisubstituted Pyrazoles

Aluminum chloride mediated reactions of N-alkylated tosylhydrazones and terminal alkynes are reported. The protocol is applied to a wide range of substrates, and demonstrates excellent functional group tolerance. A series of 1,3,5-trisubstituted pyrazoles is prepared in good to high yields with complete regioselectivity.

The preparation of substituted pyrazoles from β,β-dibromo-enones by a tandem condensation/Suzuki-Miyaura cross-coupling process

Two consecutive tandem processes are described for the regioselective, two-step synthesis of 1,3,5-trisubstituted pyrazoles from α- hydroxyketones. The first, a tandem MnO2-mediated oxidation/Ramirez olefination reaction, provides a facile route to β,β-dibromo-enones. These valuable 1,3-dicarbonyl synthons can then be converted into 1,3,5-trisubstituted pyrazoles via a second tandem hydrazine condensation/Suzuki-Miyaura cross-coupling reaction. Using these procedures, a range of aryl and alkyl α-hydroxyketones have been transformed regioselectively into 1,3,5-trisubstituted pyrazoles. Georg Thieme Verlag Stuttgart.

Aryl azoles with neuroprotective activity-Parallel synthesis and attempts at target identification

A parallel synthesis of aryl azoles with neuroprotective activity is described. All compounds obtained were evaluated in an in vitro assay using a NMDA toxicity paradigm showing a neuroprotective activity between 15% and 40%. The potential biological target of the active compounds was investigated by extensive literature searches based around similar scaffolds with reported neuroprotective activity. The most interesting molecules active in the NMDA toxicity assay (3a and 2g) showed moderate but significant activity in the inhibition of the Site 2 Sodium Channel binding assay at 10 μM. To confirm our hypothesis compounds 3a, c, f and 2g were tested in the Veratridine assay which is one of the excitotoxicity assays of revelance to NaV channels. The compounds tested showed an activity between 40% and 70%. The identification of neuroprotective small molecules and the identification of NaV channels as the potential site of action were the most important goals of this work.

Palladium-catalyzed alkynylcarbonylation of aryl iodides with the use of Mo(CO)6 in the presence of tBu3P ligand

Palladium-catalyzed alkynylcarbonylation of aryl iodides was accomplished by using Mo(CO)6 as a CO source. The reaction was conducted at room temperature with the use of tBu3P as a ligand, which was found to be essential for smooth c

Regioselective Synthesis of 1,3,5-Substituted Pyrazoles from Acetylenic Ketones and Hydrazines

The synthesis of diversely substituted 1,3,5-substituted pyrazoles from the reaction of acetylenic ketones with substituted hydrazines is reported. The reactions were shown to be highly regioselective regardless of the nature of the substituents in the su