1155811-37-2Relevant articles and documents
Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation
Peng, Lijie,Zhang, Zhensheng,Lei, Chong,Li, Shan,Zhang, Zhang,Ren, Xiaomei,Chang, Yu,Zhang, Yan,Xu, Yong,Ding, Ke
supporting information, p. 767 - 772 (2019/05/08)
A series of (E)-3-(4-((2,4-bis(trifluoromethyl)benzyl)oxy)-3-methoxyphenyl)-2-cyanoacrylamide derivatives were designed and synthesized as new estrogen-related receptor α (ERRα) degraders based on the proteolysis targeting chimera (PROTAC) concept. One of the representative compounds 6c is capable of specifically degrading ERRα protein by >80% at a relatively low concentration of 30 nM, becoming one of the most potent and selective ERRα degraders to date. Compound 6c could be utilized as a new powerful research tool for further biological investigation of ERRα.
Method for preparing 3-ketomorpholine
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Paragraph 0034; 0042; 0047-0048; 0052; 0057-0058; 0062-0078, (2019/03/26)
The invention relates to a method for preparing 3-ketomorpholine. The method comprises the following steps: protecting the amino group of ethanolamine firstly, then carrying out a reaction of amino group protected ethanolamine with alkyl haloacetate, performing deprotection on the prepared product, and performing ring closure so as to obtain 3-ketomorpholine. The method has the advantages of simple practical operation, low equipment requirements, high yield and low three waste, and is suitable for industrial large-scale production.