The use of drug-like macrocycles is emerging as an exciting area of medicinal chemistry,
with several recent examples highlighting the favorable changes in biological and …

The impressive ability of palladium to assemble CC bonds between appropriately
functionalized substrates has allowed synthetic organic chemists to perform transformations …

A new class of HCV NS3/4a protease inhibitors containing a P2 to P4 macrocyclic constraint
was designed using a molecular modeling-derived strategy. Building on the profile of …

The practices and tactics employed in successful optimizations are examined, judged from
the trajectories of ligand efficiency and property evolution. A wide range of targets is …

The discovery of asunaprevir (BMS-650032, 24) is described. This tripeptidic
acylsulfonamide inhibitor of the NS3/4A enzyme is currently in phase III clinical trials for the …

Tetrafluoroethane β-sultone (TFES) has hundreds of useful fluorinating derivatives as
reagents. The reactions of TFES with nucleophiles provide a variety of interesting …

An efficient and straightforward strategy for the synthesis of isoquinolones through [4+ 2]-
annulation of N-chlorobenzamides with vinyl acetate in the presence of CoCp*(III) catalyst in …

A strategy has been developed for the regiospecific synthesis of 1‐
trifluoromethylisoquinoline derivatives. This strategy is enabled by a photoredox vinyl …

The discovery of BMS-605339 (35), a tripeptidic inhibitor of the NS3/4A enzyme, is
described. This compound incorporates a cyclopropylacylsulfonamide moiety that was …

Due to the unique role of l-proline in the folding and structure of protein, a variety of synthetic
proline analogues have been developed. l-Proline analogues have been proven to be …