223526-96-3Relevant academic research and scientific papers
Reverse regioselection in the synthesis of spiropyrazolobarbiturates using C-Br and C-H nitrilimines
Foti, Francesco,Grassi, Giovanni,Risitano, Francesco
, p. 125 - 126 (2005)
The 1,3-dipolar cycloaddition of arylmethylenebarbiturates 4 with C-Br 2 and C-H 3 nitrilimines gives spiropyrazolobarbiturates 5 and 6 with reverse regioselectivities.
First synthesis of a bromonitrilimine. Direct formation of 3- bromopyrazole derivatives
Foti, Francesco,Grassi, Giovanni,Risitano, Francesco
, p. 2605 - 2606 (1999)
The first example of the preparation of bromonitrilimine 3 is described. This precursor provides a convenient entry to a highly regioselective synthesis of 3-bromopyrazole derivatives 4 and 5.
Design, synthesis and biological activity of novel substituted pyrazole amide derivatives targeting EcR/USP receptor
Deng, Xi-Le,Xie, Jin,Li, Yong-Qiang,Yuan, De-Kai,Hu, Xue-Ping,Zhang, Li,Wang, Qing-Min,Chi, Ming,Yang, Xin-Ling
supporting information, p. 566 - 570 (2016/04/26)
In order to discover highly active ecdysone analogs, a series of new substituted pyrazole amide derivatives were obtained using structure-guided optimization method and further screened for their insecticidal activities, in the basis of the core structures of the two active compounds N-(3-methoxyphenyl)-3-(tert-butyl)-1-phenyl-1H-pyrazole-5-carboxamide (6e) and N-(4-(tert-butyl)phenyl)-3-(tert-butyl)-1-phenyl-1H-pyrazole-5-carboxamide (6i), previously presented by us. The chemical structures of the title compounds were identified by spectral analyses. The preliminary bioassay results indicated that one among the synthesized pyrazole derivatives, compound 34, endowed with good activity against Mythimna Separata at 10 mg/L, which was equal to that displayed by the positive control tebufenozide. In addition, examples of molecular docking and molecular dynamics studies demonstrated that 34 may be the potential inhibitor to EcR and its docking conformation was similar to that of tebufenozide. In addition, increasing the hydrophobic effect and considering the suitable bulk effect on pyrazole ring are beneficial to the inhibiting activity to EcR and activity in vivo.
Synthesis of pyrazolinyl heterocycles via adenine- or imidazole-containing nitrilimine cycloaddition
Foti, Francesco,Grassi, Giovanni,Liotta, Claudia,Risitano, Francesco
, p. 1730 - 1732 (2008/02/07)
Pyrazolinyl nucleoside analogues via adenine- or imidazole-containing nitrilimine cycloaddition have been prepared. The key feature of our synthetic strategy is the introduction of the base moiety through the new 1,3-dipole. Georg Thieme Verlag Stuttgart.
