in addition to a small amount of demethoxylated naphthofuran II and benzoindolinone III (Scheme 1, eq. 1). Although the yield of the heterocyclic compounds II and III was poor, the carbon-carbon bond formation efficiently occurred during the reaction. We also reported the facile synthesis of 3,4-dihydro-2(1H)-quinolinones, 540 HETEROCYCLES, Vol. 90, No. 1, 2015
Two Consecutive Palladium(II)-Promoted CH Alkenylation Reactions for the Synthesis of 3-Alkenylquinolones
作者:Verónica Ortiz-de-Elguea、Nuria Sotomayor、Esther Lete
DOI:10.1002/adsc.201400931
日期:2015.2.9
AbstractHighly substituted quinolones are obtained through an efficient and atom economical procedure that involves two consecutive palladium(II)‐catalyzed CH alkenylation reactions. A selective 6‐endo intramolecular CH alkenylation leads to 4‐substituted quinolones that have been further functionalized at C‐3 through a second intermolecular CH alkenylation reaction.magnified image
Stereospecific Copper-Catalyzed Domino Ring Opening and sp<sup>3</sup> C–H Functionalization of Activated Aziridines with <i>N</i>-Alkylanilines
Copper efficiently catalyzed nucleophilic ring opening, sp(3) C-H functionalization, and C-N bond formation in the presence of tert-butyl hydroperoxide to afford functionalized imidazolidines starting from N-sulfonylaziridines and N-alkylanilines. The products were obtained in high optical purities (95 -> 99% ee) with excellent functional group tolerance.
INHIBITORS OF SERINE PROTEASES, PARTICULARLY HEPATITIS C VIRUS NS3 PROTEASE
申请人:Tung Roger D.
公开号:US20090143312A1
公开(公告)日:2009-06-04
The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.