403705-10-2Relevant articles and documents
Synthesis of a selective estrogen receptor degrader via a stereospecific elimination approach
Lim, Ngiap-Kie,Cravillion, Theresa,Savage, Scott,McClory, Andrew,Han, Chong,Zhang, Haiming,Dipasquale, Antonio,Gosselin, Francis
, p. 1114 - 1117 (2018)
An efficient synthesis of a selective estrogen receptor degrader, GDC-0810, bearing a challenging stereodefined (E)-tetrasubstituted all-carbon olefin core, is reported. The described synthetic route involves a highly diastereoselective addition of an ary
Improving reactivity and selectivity of aqueous-based Heck reactions by the local hydrophobicity of phosphine ligands
Roberts, Gina M.,Zhang, Shiyong,Zhao, Yan,Woo, L. Keith
, p. 8263 - 8270 (2015/10/05)
Modification of a triarylphosphine with a cholate moiety affords a new ligand, 1, which is effective in palladium-catalyzed Heck cross-couplings between acrylates and aryl iodides under mild, aqueous reaction conditions. High yields, up to 99%, were achieved in water at 40 °C. In competition studies, a more hydrophobic substrate (n-Bu acrylate) was preferred over the least hydrophobic substrate (methyl acrylate), supportive of a localized hydrophobic microenvironment near the catalytic center. The enhanced reactivity and selectivity for hydrophobic substrates disappeared when the local hydrophobicity was eliminated using a standard water-soluble phosphine or in organic solvents.
ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
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Paragraph 00530, (2013/10/08)
Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
