121069-00-9Relevant articles and documents
Electrochemical synthesis of α,α-dihaloacetophenones from terminal alkyne derivatives
Li, Zhibin,Sun, Qi,Qian, Peng,Hu, Kangfei,Zha, Zhenggen,Wang, Zhiyong
, p. 1855 - 1858 (2020)
By virtue of electrochemistry, a series of α,α-dihaloacetophenones were easily obtained with good to excellent yields. This electrochemical procedure was taken in a divided cell with constant current in aqueous media. The reaction can be carried out smoothly at room temperature under metal and oxidant free condition, which provides an eco-friendly synthesis for the α,α-dihaloacetophenone derivatives.
Dichloroacetophenones targeting at pyruvate dehydrogenase kinase 1 with improved selectivity and antiproliferative activity: Synthesis and structure-activity relationships
Zhang, Shao-Lin,Yang, Zheng,Hu, Xiaohui,Tam, Kin Yip
supporting information, p. 3441 - 3445 (2018/09/29)
Dichloroacetophenone is a pyruvate dehydrogenase kinase 1 (PDK1) inhibitor with suboptimal kinase selectivity. Herein, we report the synthesis and biological evaluation of a series of novel dichloroacetophenones. Structure-activity relationship analyses (SARs) enabled us to identify three potent compounds, namely 54, 55, and 64, which inhibited PDK1 function, activated pyruvate dehydrogenase complex, and reduced the proliferation of NCI-H1975 cells. Mitochondrial bioenergetics assay suggested that 54, 55, and 64 enhanced the oxidative phosphorylation in cancer cells, which might contribute to the observed anti-proliferation effects. Collectively, these results suggested that 54, 55, and 64 could be promising compounds for the development of potent PDK1 inhibitors.
Halogenation Using Quaternary Ammonium Polyhalides. XXXII. Dichlorination of Aromatic Acetyl Derivatives with Benzyltrimethylammonium Tetrachloroiodate
Kakinami, Takaaki,Urabe, Yasuaki,Hermawan, Irwan,Yamanishi, Hiroko,Okamoto, Tsuyoshi,Kajigaeshi, Shoji
, p. 2549 - 2551 (2007/10/02)
The reaction of aromatic acetyl derivatives with 2 molar amounts of benzyltrimethylammonium tetrachloroiodate in acetic acid at 70 deg C for several hours gave dichloroacetyl derivatives in good yields.