1785580-89-3Relevant academic research and scientific papers
N/O-LINKED DEGRONS AND DEGRONIMERS FOR PROTEIN DEGRADATION
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Page/Page column 326, (2019/01/10)
This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.
Strategy to Prepare 3-Bromo- and 3-Chloropyrazoles
Fox, Richard J.,Schmidt, Michael A.,Eastgate, Martin D.
, p. 2830 - 2839 (2018/03/09)
A general strategy to prepare substituted 3-bromo- and 3-chloropyrazoles is described. The three-step method involves condensation of crotonates or β-chloro carboxylic acids with hydrazines, followed by halogenation and oxidation. Several condensation and oxidation protocols were developed to enable preparation of a wide variety of 3-halopyrazoles with good to excellent yields and regiocontrol.
