5456-52-0Relevant academic research and scientific papers
Design, synthesis and biological evaluation of selective histone deacetylase 6 (HDAC6) inhibitors bearing benzoindazole or pyrazoloindazole scaffold as surface recognition motif
Xu, Qihao,Mou, Yanhua,Wang, Siyuan,Gao, Xiaoxiao,Zhang, Yulong,Wang, Zhi,Xu, Xiangwei,Han, Yu,Jia, Wenlong,Zhang, Meihui,Zhao, Linxiang,Liu, Dan
, (2021/04/27)
A series of compounds were designed and synthesized based on the compound 11i bearing phenylpyrazole scaffold with histone deacetylase 6 (HDAC6) inhibitory activity. Most of the compounds showed considerable inhibitory activity against HDAC6 and compound
Gold-catalyzed ring-expansion through acyl migration to afford furan-fused polycyclic compounds
Zhang, Changyuan,Jiang, Huanfeng,Zhu, Shifa
supporting information, p. 2677 - 2680 (2017/03/10)
A gold-catalyzed ring-expansion reaction of alkynones to access furan-fused polycyclic compounds is reported. Mechanistic studies revealed that the reaction might occur through a tandem 1,2-acyl migration/Friedel-Crafts reaction.
Trimethylchlorosilane-Mediated Mild α-Chlorination of 1,3-Dicarbonyl Compounds Promoted by Phenyliodonium Diacetate
Chong, Siying,Su, Yingpeng,Wu, Lili,Zhang, Weigang,Ma, Junyan,Chen, Xiaowei,Huang, Danfeng,Wang, Ke-Hu,Hu, Yulai
supporting information, p. 1359 - 1370 (2016/05/02)
Trimethylchlorosilane was used as chlorine source for the α-chlorination of 1,3-dicarbonyl compounds with phenyliodonium diacetate as oxidant at room temperature. The reaction allows the selective synthesis of α-monochlorinated products from different kinds of 1,3-dicarbonyl compounds in good yield. The potential possibility of this conversion for bromination has also been investigated.
Variations in the blaise reaction: Conceptually new synthesis of 3-amino enones and 1,3-diketones
Rao, H. Surya Prakash,Muthanna, Nandurka
supporting information, p. 1525 - 1532 (2015/03/04)
Organic compounds with 3-amino enone or 1,3-diketone functional groups are extremely important, as they can be converted into a plethora of heterocyclic or carbocyclic compounds, or can be used as ligands in metal complexes. We have achieved a new, easy, straightforward and convenient synthesis of 3-amino enones and 1,3-diketones starting from aryl/heteroaryl/alkyl nitriles and 1-aryl/alkyl 2-bromoethanones. The reaction is a variation of the classical Blaise reaction, and it works with zinc and trimethylsilyl chloride as an activator. By running the hydrolysis of the reaction intermediate with HCl (3 N aq.) at 0-30 °C or at 100 °C, it is possible to form either 3-amino enones or 1,3-diketones, respectively. The newly developed method was used for the synthesis of avobenzone, an ingredient of sun-screen lotions. Furthermore, an easy synthesis of (Z)-3-amino-1-[4-(tertbutyl) phenyl]-3-(4-methoxyphenyl)prop-2-en-1-one, with UV/Vis absorption characteristics similar to those of avobenzone, was also achieved.
SAR-based optimization of 2-(1H-pyrazol-1-yl)-thiazole derivatives as highly potent EP1 receptor antagonists
Atobe, Masakazu,Naganuma, Kenji,Kawanishi, Masashi,Morimoto, Akifumi,Kasahara, Ken-Ichi,Ohashi, Shigeki,Suzuki, Hiroko,Hayashi, Takahiko,Miyoshi, Shiro
, p. 6569 - 6576 (2014/01/06)
We describe a medicinal chemistry approach for generating a series of 2-(1H-pyrazol-1-yl)thiazoles as EP1 receptor antagonists. To improve the physicochemical properties of compound 1, we investigated its structure-activity relationships (SAR).
Synthesis of chiral 2-aroyl-1-tetralols: Asymmetric transfer hydrgenation of 2-aroyl-1-tetralones via dynamic kinetic resolution
Wu, Yun,Geng, Zhicong,Bai, Jinjin,Zhang, Yawen
, p. 1467 - 1472 (2011/11/05)
The dynamic kinetic resolution of 2-aroyl-1-tetralones was achieved via asymmetric transfer hydrogenation using (S,S)-RuCl(p-cymene)TsDPEN (TsDPEN=N-(tosyl)-1,2-diphenylethylenediamine) in formic acid/triethyl- amine (5:2, molar ratio), afforded the desired products in good yields (up to 85%) with diastereomeric ratio up to >99:1 and high enantiomeric excesses (up to >99%). The absolute configuration of major the product was confirmed by X-ray crystal structure analysis. Copyright
