558644-29-4Relevant academic research and scientific papers
Heck Reactions of Acrolein or Enones and Aryl Bromides – Synthesis of 3-Aryl Propenals or Propenones and Consecutive Application in Multicomponent Pyrazole Syntheses
Stephan, Marvin,Panther, Jesco,Wilbert, Fabio,Ozog, Pauline,Müller, Thomas J. J.
, p. 2086 - 2092 (2020/03/23)
3-(Hetero)aryl propenals or propenones are efficiently prepared by a Heck reaction of (hetero)aryl bromides and acrolein or vinyl ketones using Beller's CataCXium Ptb ligand under Jeffery's and Fu's conditions. The formation of these three-carbon building blocks is embedded into consecutive three- and pseudo-four-component syntheses of 3-(hetero)aryl and 3,5-diarylpyrazoles with a broad substitution pattern in moderate to excellent yield.
Design, synthesis, and biological evaluation of 2-(5-methyl-1H-pyrazol-1-yl) acetamide derivatives as androgen receptor antagonists
Dong, Junze,Zhang, Jingya,Li, Zilu,Asnake, Solomon,Zhang, Daoguang,Olsson, Per-Erik,Zhao, Guisen
, p. 380 - 386 (2019/01/30)
Androgen receptor (AR) signaling is often activated in prostate cancer (PCa) cells, and blockage of this signaling by AR antagonists is an important strategy in PCa therapy. In this study, we designed and synthesized a series of 2-(5-methyl-1H-pyrazol-1-y
Discovery of novel 5-methyl-1H-pyrazole derivatives as potential antiprostate cancer agents: Design, synthesis, molecular modeling, and biological evaluation
Zhang, Daoguang,Asnake, Solomon,Zhang, Jingya,Olsson, Per-Erik,Zhao, Guisen
, p. 1113 - 1124 (2018/03/05)
Androgen receptor (AR) signaling functions as a core driving force for the progression of prostate cancer (PCa), and AR has been proved to be an effective therapeutic target even for castration-resistant prostate cancer (CRPC). Herein, structural modification via a fragments splicing strategy was performed based on two lead compounds T3 and 10e, leading to the discovery of a series of 5-methyl-1H-pyrazole derivatives. AR reporter gene assay revealed compounds A13 and A14 as potent AR antagonists. Some of the compounds in this series inhibited growth of PCa LNCaP cells more efficiently than enzalutamide. A13 and A14 also showed improved metabolic stability compared with 10e in human liver microsomes.
5-methyl-1H-pyrazole derivative, preparation method and applications thereof
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Paragraph 0060-0064, (2018/05/01)
The invention discloses a 5-methyl-1H-pyrazole derivative, a preparation method and applications thereof, wherein the compound has a structure represented by a general formula (I). The invention further provides the preparation method and the applications
1,3-disubstituted pyrazole derivative as well as preparation method and application thereof
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Paragraph 0093; 0094; 0095; 0096, (2018/03/24)
The invention discloses a 1,3-disubstituted pyrazole derivative as well as a preparation method and application thereof. The compound has a structure shown as a general formula (I). The invention further provides a preparation method of the compounds and
A simple and efficient synthesis of pyrazoles in water
Wen, Jun,Fu, Yun,Zhang, Ruo-Yi,Zhang, Ji,Chen, Shan-Yong,Yu, Xiao-Qi
, p. 9618 - 9621 (2011/12/14)
A simple, highly efficient, and environmentally friendly method for the synthesis of substituted 1H-pyrazoles by one-pot condensation reaction of α,β-unsaturated carbonyl compounds with tosyl hydrazide in water was developed. The reaction system exhibited tolerance with various functional groups, Aromatic moiety with both electron-rich and electron-deficient substituents could give desired products in good to excellent yields.
