56119-89-2Relevant academic research and scientific papers
Preparation method for pyrazole
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Paragraph 0011; 0012; 0013; 0014; 0015; 0016; 0129; 0130, (2017/08/26)
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
Tang, Meng,Wang, Yun,Wang, Hu,Kong, Yuanfang
, p. 3065 - 3076 (2016/09/09)
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.
Regioselective synthesis of 1,3,5-Trisubstituted Pyrazoles from N-Alkylated Tosylhydrazones and terminal Alkynes
Kong, Yuanfang,Tang, Meng,Wang, Yun
, p. 576 - 579 (2014/04/03)
An efficient synthesis of 1,3,5-trisubstituted pyrazoles from Nalkylated tosylhydrazones and terminal alkynes was developed. The protocol was applied to a wide range of substrates and demonstrated excellent tolerance to a variety of substituents, includin
Rapid one-pot, four-step synthesis of highly fluorescent 1,3,4,5-tetrasubstituted pyrazoles
Willy, Benjamin,Mueller, Thomas J.J.
, p. 2082 - 2085 (2011/06/24)
1,3,4,5-Tetrasubstituted pyrazoles can be rapidly and efficiently synthesized in a one-pot, four-step sequence consisting of Sonogashira coupling, addition-cyclocondensation, bromination, and Suzuki coupling. The second and the last step are microwave-ass
Regioselective three-component synthesis of highly fluorescent 1,3,5-trisubstituted pyrazoles
Willy, Benjamin,Mueller, Thomas J. J.
experimental part, p. 4157 - 4168 (2009/05/11)
3,5-Disubstituted and 1,3,5-trisubstituted pyrazoles are readily synthesized from acyl chlorides, terminal alkynes, and hydrazines by a consecutive one-pot three-component Sonogashira coupling/Michael addition/cyclocondensation sequence in good to excelle
Aryl azoles with neuroprotective activity-Parallel synthesis and attempts at target identification
Cocconcelli, Giuseppe,Diodato, Enrica,Caricasole, Andrea,Gaviraghi, Giovanni,Genesio, Eva,Ghiron, Chiara,Magnoni, Letizia,Pecchioli, Elena,Plazzi, Pier Vincenzo,Terstappen, Georg C.
, p. 2043 - 2052 (2008/09/21)
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.
Regioselective Synthesis of 1,3,5-Substituted Pyrazoles from Acetylenic Ketones and Hydrazines
Bishop, Brian C.,Brands, Karel M. J.,Gibb, Andrew D.,Kennedy, Derek J.
, p. 43 - 52 (2007/10/03)
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
