39143-05-0Relevant academic research and scientific papers
Highly stereoselective construction of spiro[cyclopropane-1,4′-pyrazolin-5′-one]with 4-arylidene-3-methyl-1-phenyl-pyrazolin-5-one and arsonium ylide
Ren, Zhongjiao,Cao, Weiguo,Chen, Jie,Chen, Yali,Deng, Hongmei,Shao, Min,Wu, Danyi
, p. 5156 - 5161 (2008)
A highly stereoselective synthesis of exo-spiro[cyclopropane-1,4′-pyrazolin-5′-one] from 4-arylidene-3-methyl-1-phenyl-pyrazolin-5-one and arsonium bromide in the presence of base has been achieved. The triphenylarsine-catalyzed cyclopropanation of 4-arylidene-3-methyl-1-phenyl-pyrazolin-5-one with bromide in the presence of NaHCO3 has also been studied. Both exo and endo isomers were formed in this reaction. The structures of the products were characterized by IR, MS, 1H NMR, elemental analysis, and X-ray diffraction analysis.
Organophosphane-catalyzed direct β-acylation of 4-arylidene pyrazolones and 5-arylidene thiazolones with acyl chlorides
Khairnar, Pankaj V.,Su, Yin-Hsiang,Chen, Yung-Chang,Edukondalu, Athukuri,Chen, Yi-Ru,Lin, Wenwei
supporting information, p. 6868 - 6872 (2020/09/15)
An efficient method for the direct β-acylation of arylidene pyrazolones and thiazolones with acyl chlorides in the presence of a base catalyzed by organophosphanes is reported. A variety of functionalized 4-arylidene pyrazolone and 5-arylidene thiazolone derivatives were prepared under metal-free and mild conditions via a tandem phospha-Michael addition/O-acylation/intramolecular cyclization/rearrangement sequence. Our mechanistic investigations revealed that the reaction is highly stereospecific to provide exclusively cis-isomers, and the methodology can also be scaled up with similar efficacy.
An asymmetric approach toward chiral multicyclic spirooxindoles from isothiocyanato oxindoles and unsaturated pyrazolones by a chiral tertiary amine thiourea catalyst
Chen, Qiao,Liang, Jinyan,Wang, Shoulei,Wang, Dong,Wang, Rui
supporting information, p. 1657 - 1659 (2013/03/14)
The first organocatalytic Michael-cyclization cascade reaction between isothiocyanato oxindoles and unsaturated pyrazolones has been developed. The multicyclic spiro[oxindole/thiobutyrolactam/pyrazolone] core structures containing three contiguous stereog
Discovery and optimization of 1,3,4-trisubstituted-pyrazolone derivatives as novel, potent, and nonsteroidal farnesoid X receptor (FXR) selective antagonists
Huang, Huang,Yu, Ying,Gao, Zhenting,Jin, Hui,Yan, Wenzhong,Ma, Ruoqun,Zhu, Jin,Shen, Xu,Jiang, Hualiang,Li, Jian,Li, Chenjing,Xu, Xing,Chen, Lili,Zhang, Yong
, p. 7037 - 7053,17 (2012/12/11)
LBVS of 12480 in-house compounds, followed by HTRF assay, resulted in one nonsteroidal compound (11) with antagonistic activity against FXR (69.01 ± 11.75 μM). On the basis of 11, 26 new derivatives (12a-z) were designed and synthesized accordingly. Five
Discovery and optimization of 1,3,4-trisubstituted-pyrazolone derivatives as novel, potent, and nonsteroidal farnesoid X receptor (FXR) selective antagonists
Huang, Huang,Yu, Ying,Gao, Zhenting,Zhang, Yong,Li, Chenjing,Xu, Xing,Jin, Hui,Yan, Wenzhong,Ma, Ruoqun,Zhu, Jin,Shen, Xu,Jiang, Hualiang,Chen, Lili,Li, Jian
, p. 7037 - 7053 (2013/01/14)
LBVS of 12480 in-house compounds, followed by HTRF assay, resulted in one nonsteroidal compound (11) with antagonistic activity against FXR (69.01 ± 11.75 μM). On the basis of 11, 26 new derivatives (12a-z) were designed and synthesized accordingly. Five
Oxopyrazoline-spiro-oxirans. A New Class of Reactive Heterocycles
Ege, Seyhan N.,Adams, Alan. D.,Gess, E. Joseph,Ragone, Katherine S.,Kober, Brian J.,et al.
, p. 325 - 332 (2007/10/02)
Chemical and spectral properties of a series of 1-oxa-5,6-diazaspirohept-6-en-4-ones, synthesized by the oxidation of 4-alkylidene- or 4-arylidene-1-aryl-2-pyrazolin-5-ones are reported
