94206-50-5Relevant academic research and scientific papers
Ligand-Dependent Site-Selective Suzuki Cross-Coupling of 4-Bromopyrazol-5-yl Triflates
Sakakibara, Ryo,Itoh, Kennosuke,Fujii, Hideaki
, p. 11474 - 11481 (2019/08/20)
Ligand-dependent Suzuki cross-coupling of 4-bromopyrazol-5-yl triflates has been developed. This approach enabled selective introduction of an aryl substituent at the C4 or C5 position in pyrazoles. This protocol is the first example in which the cross-coupling proceeded predominantly at the C4 position in pyrazoles, which is generally recognized as the least reactive position. The selection of phosphine ligands switched the order of arylation. This method should be highly useful for preparing diverse poly-substituted pyrazole derivatives.
Copper-catalyzed aerobic C(sp2)-H functionalization for C-N bond formation: Synthesis of pyrazoles and indazoles
Li, Xianwei,He, Li,Chen, Huoji,Wu, Wanqing,Jiang, Huanfeng
, p. 3636 - 3646 (2013/06/04)
A simple, practical, and highly efficient synthesis of pyrazoles and indazoles via copper-catalyzed direct aerobic oxidative C(sp2)-H amination has been reported herein. This process tolerated a variety of functional groups under mild conditions. Further diversification of pyrazoles was also investigated, which provided its potential for drug discovery.
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: Lead identification and SAR of 3- and 4-substituted derivatives
Genin, Michael J.,Biles, Carolyn,Keiser, Barb J.,Poppe, Susan M.,Swaney, Steven M.,Tarpley, W. Gary,Yagi, Yoshihiko,Romero, Donna L.
, p. 1034 - 1040 (2007/10/03)
Through computationally directed broad screening, a novel 1,5- diphenylpyrazole (DPP) class of HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) has been discovered. Compound 2 (PNU-32945) was found to have good activity versus wild-type (ICs
