444643-83-8Relevant academic research and scientific papers
Nickel-Mediated Trifluoromethylation of Phenol Derivatives by Aryl C?O Bond Activation
Hu, Wei-Qiang,Pan, Shen,Qing, Feng-Ling,Vicic, David A.,Xu, Xiu-Hua
supporting information, p. 16076 - 16082 (2020/07/04)
The increasing pharmaceutical importance of trifluoromethylarenes has stimulated the development of more efficient trifluoromethylation reactions. Tremendous efforts have focused on copper- and palladium-mediated/catalyzed trifluoromethylation of aryl halides. In contrast, no general method exists for the conversion of widely available inert electrophiles, such as phenol derivatives, into the corresponding trifluoromethylated arenes. Reported herein is a practical nickel-mediated trifluoromethylation of phenol derivatives with readily available trimethyl(trifluoromethyl)silane (TMSCF3). The strategy relies on PMe3-promoted oxidative addition and transmetalation, and CCl3CN-induced reductive elimination. The broad utility of this transformation has been demonstrated through the direct incorporation of trifluoromethyl into aromatic and heteroaromatic systems, including biorelevant compounds.
Synthesis, pharmacological evaluation, and structure-activity relationships of benzopyran derivatives with potent SERM activity
Amari, Gabriele,Armani, Elisabetta,Ghirardi, Silvia,Delcanale, Maurizio,Civelli, Maurizio,Caruso, Paola Lorenza,Galbiati, Elisabetta,Lipreri, Milco,Rivara, Silvia,Lodola, Alessio,Mor, Marco
, p. 3763 - 3782 (2007/10/03)
The synthesis, binding affinity for estrogen receptor subtypes (ERα and ERβ) and pharmacological activity on rat uterus of a new class of potent ligands, characterized by a 3-phenylbenzopyran scaffold with a basic side chain in position 4, are reported. S
