2606-57-7Relevant articles and documents
Synthetic method for dapagliflozin
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Paragraph 0015; 0016, (2018/03/26)
The invention relates to a synthetic method for dapagliflozin. The synthetic method is characterized in that 4-methylphenol is taken as a starting raw material, alkylation and bromination are performed, an alkylation reaction is performed with antisepsin, diazotization and chlorination are performed, and condensation, etherification and desmethoxy are performed with 2,3,4,6-tetrakis-O-trimethylsilyl-D-gluconolactone to obtain a hypoglycemic drug (dapagliflozin). The synthetic method has the following advantages: 4-methylphenol is taken as the starting raw material, and 4-methylphenol is low inprice and easily accessible than 5-bromo-2-chlorobenzoic acid; by adoption of the process, industrialization can be easily realized; in the synthesis process, raw materials which are highly toxic arenot used, so that dangerous processes are avoided; the synthesis path is short and novel, so that the operation is simple and convenient; and by adoption of the synthesis path, the purity of a finalproduct can be improved, and the purity can be 99% or above.
Synthesis and biological evaluation of aryloxyacetamide derivatives as neuroprotective agents
Zhong, Yan,Xu, Yi,Zhang, Ai-Xia,Li, Xiao-Feng,Xu, Zhao-Ying,Li, Ping,Wu, Bin
, p. 2526 - 2530 (2016/07/07)
A series of new aryloxyacetamide derivatives 10a-s and 14a-m are designed and synthesized. Their protective activities against the glutamate-induced cell death were investigated in differentiated rat pheochromocytoma cells (PC12 cells). Most compounds exhibited neuroprotective effects, especially for 10m, 10r, 14b and 14c, which showed potential protection of PC12 cells at three doses (0.1, 1.0, 10 μM). MTT assay, Hoechst 33342/PI double staining, and high content screening (HCS) revealed that pretreatment of the cells with 10m, 10r, 14b and 14c has significantly decreased the extent of cell apoptosis in a dose-dependent manner. The results of western blot analysis demonstrated these compounds suppressed apoptosis of glutamate-induced PC12 cells via caspase-3 pathway. These compounds can be lead compounds for further discovery of neuroprotective agents for treating cerebral ischemic stroke. Basic structure-activity relationships are also presented.
INHIBITORS OF ACETYL-COA CARBOXYLASE
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Page/Page column 62-63, (2010/11/17)
The present invention relates to compounds that act as acetyl-CoA carboxylase (ACC) inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.