66127-06-8Relevant academic research and scientific papers
Halotrifluoromethylation of 1,3-Enynes: Access to Tetrasubstituted Allenes
Huang, Jinfeng,Jia, Yimin,Li, Xiangyu,Duan, Jianli,Jiang, Zhong-Xing,Yang, Zhigang
supporting information, p. 2314 - 2319 (2021/04/05)
A highly regioselective copper-catalyzed 1,4-chloro- and bromotrifluoromethylation of 1,3-enynes has been presented for the first time, which affords an efficient transformation to access halo- and CF3-containing tetrasubstituted allene derivatives with good to excellent yield. This protocol is practical and convenient, in which a wide range of functional groups are compatible. Applications of this method for the gram-scale preparation and late-stage functionalization of biologically active molecules are also demonstrated.
Discovery of α,γ-Diketo Acids as Potent Selective and Reversible Inhibitors of Hepatitis C Virus NS5b RNA-Dependent RNA Polymerase
Summa, Vincenzo,Petrocchi, Alessia,Pace, Paola,Matassa, Victor G.,De Francesco, Raffaele,Altamura, Sergio,Tomei, Licia,Koch, Uwe,Neuner, Philippe
, p. 14 - 17 (2007/10/03)
α,γ-Diketo acids (DKA) were discovered from screening as selective and reversible inhibitors of hepatitis C virus NS5b RNA-dependent RNA polymerase. The diketo acid moiety proved essential for activity, while substitution on the γ position was necessary for selectivity and potency. Optimization led to the identification of a DKA inhibitor of NS5b polymerase with IC50 = 45 nM, one of the most potent HCV NS5b polymerase inhibitors reported.
