82082-50-6Relevant articles and documents
Structure-Activity Studies Reveal Scope for Optimisation of Ebselen-Type Inhibition of SARS-CoV-2 Main Protease
Thun-Hohenstein, Siegfried T. D.,Suits, Timothy F.,Malla, Tika R.,Tumber, Anthony,Brewitz, Lennart,Choudhry, Hani,Salah, Eidarus,Schofield, Christopher J.
, (2021/12/30)
The reactive organoselenium compound ebselen is being investigated for treatment of coronavirus disease 2019 (COVID-19) and other diseases. We report structure-activity studies on sulfur analogues of ebselen with the Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), employing turnover and protein-observed mass spectrometry-based assays. The results reveal scope for optimisation of ebselen/ebselen derivative- mediated inhibition of Mpro, particularly with respect to improved selectivity.
Rapid construction of C4-substituted phenanthridinones through palladium-catalyzed domino N-arylation/aryl-aryl coupling process
Liu, Chao,Song, Liangliang,Van Meervelt, Luc,Van der Eycken, Erik V.
, (2021/08/05)
An excellent chemo- and regioselective palladium-catalyzed cascade intermolecular N-arylation/aryl-aryl coupling process has been developed. Employing Pd(TFA)2, PCy3?HBF4, K2CO3 and 1,4-dioxane in an oil bath at 100°C for 12 h, diverse C4-substituted phenanthridinones are synthesized from o-bromobenzamides in 42-92% yield. Broad substrate scope and excellent functional group tolerance are observed. The synthetic utility of this method is illustrated by the further derivatization to prepare multiple-substituted phenanthridinones in 30-75% yield.
A solid-supported arylboronic acid catalyst for direct amidation
Du, Yihao,Barber, Thomas,Lim, Sol Ee,Rzepa, Henry S.,Baxendale, Ian R.,Whiting, Andrew
supporting information, p. 2916 - 2919 (2019/03/27)
An efficient heterogeneous amidation catalyst has been prepared by co-polymerisation of styrene, DVB with 4-styreneboronic acid, which shows wide substrate applicability and higher reactivity than the equivalent homogeneous phenylboronic acid, suggesting potential cooperative catalytic effects. The catalyst can be easily recovered and reused; suitable for use in packed bed flow reactors.