Robert E. Kyne

TL;DR: The Pd-catalyzed cross-coupling of racemic tertiary allylic carbonates and allylboronates is described, which generates all-carbon quaternary centers in a highly regioselective and enantioselectives fashion.

TL;DR: This work describes the first rational targeting of tyrosine residues in a protein binding site by small-molecule covalent probes, illustrating the utility of sulfonyl fluoride probes designed to react with specific tyrosines of a protein and augments the chemical biology toolkit by these probes uses in target validation and molecular pharmacology.

TL;DR: A fluorosulfate-containing inhibitor with excellent chemical and metabolic stability that reacts selectively with a noncatalytic serine residue in the same active site of DcpS is described as confirmed by peptide mapping experiments and suggests that nonCatalytic Serine targeting using fluoros sulfurate electrophilic warheads could be a suitable strategy for the development of covalent inhibitor drugs and chemical probes.

TL;DR: This annual review covers the synthesis of twenty-four NCEs that were approved for the first time in 2013 and two 2012 drugs which were not covered during the previous edition of this review.

TL;DR: 1,3-Diols engage in ruthenium-catalyzed hydrogen transfer in the presence of alkyl hydrazines to provide 1,4-disubstituted pyrazoles to enable regioselective synthesis of unsymmetrical pyrazole from β-hydroxy ketones.