352525-97-4Relevant academic research and scientific papers
Copper-catalyzed oxyvinylation of diazo compounds
Pisella, Guillaume,Gagnebin, Alec,Waser, Jerome
supporting information, p. 3884 - 3889 (2020/05/14)
A copper(I)-catalyzed vinylation of diazo compounds with vinylbenziodoxolone reagents (VBX) as partners is reported. The transformation tolerates diverse functionalities on both reagents delivering polyfunctionalized vinylated products. The strategy was successfully extended to a three-component/intermolecular version with alcohols. The obtained products contain synthetically versatile functional groups, such as an aryl iodide, an ester, and an allylic leaving group, enabling further modification.
Synthesis and evaluation of 4-(substituted styryl/alkenyl)-3,5-bis(4- hydroxyphenyl)-isoxazoles as ligands for the estrogen receptor
Haddad, Terra,Gershman, Rachel,Dilis, Robert,Hanson, Robert N.,Labaree, David,Hochberg, Richard B.
supporting information, p. 5999 - 6003,5 (2020/07/31)
A series of 3,5-bis (4-hydroxyphenyl) isoxazoles bearing a styryl/alkyl vinyl group at the 4-position were prepared and evaluated as ligands for the estrogen receptor-alpha (ERα). The target compounds were prepared using the Suzuki reaction to couple an iodo-isoxazole intermediate with a series of styryl/alkenyl boronic acids, followed by O-demethylation. The products were evaluated for their estrogen receptor-α ligand binding domain (ERα-LBD) binding affinity using a competitive binding assay. The 4-(4-hydroxystyryl) derivative 4 h displays binding properties similar to those of the previously described pyrazole class of ER ligands, indicating that the ERα-LBD tolerates the presence of the added vinyl group at the 4-position of the isoxazole ring.
