Remote Alkynylation of Aliphatic Amines.

Advancements in transition metal catalyzed C-H activation/functionalization cascades have allowed the synthetic chemist's toolbox to be significantly expanded. Despite this, protocols for the remote alkynylation of linear aliphatic amines still remain limited. Herein, a palladium-catalyzed directing-group approach to alkynylation of aliphatic amines is disclosed.

Discovery and structure-activity relationships of a novel oxazolidinone class of bacterial type II topoisomerase inhibitors.

There is an increasingly urgent and unmet medical need for novel antibiotic drugs that tackle infections caused by multidrug-resistant (MDR) pathogens. Novel bacterial type II topoisomerase inhibitors (NBTIs) are of high interest due to limited cross-resistance with fluoroquinolones, however analogues with Gram-negative activity often suffer from hERG channel inhibition. A novel series of bicyclic-oxazolidinone inhibitors of bacterial type II topoisomerase were identified which display potent broad-spectrum anti-bacterial activity, including against MDR strains, along with an encouraging in vitro safety profile.

A dual photoredox-nickel strategy for remote functionalization iminyl radicals: radical ring-opening-arylation, -vinylation and -alkylation cascades.

A divergent strategy for the remote arylation, vinylation and alkylation of nitriles is described. These processes proceed through the photoredox generation of a cyclic iminyl radical and its following ring-opening reaction. The distal nitrile radical is then engaged in nickel-based catalytic cycles to form C-C bonds with aryl bromides, alkynes and alkyl bromides.

Correction: A dual photoredox-nickel strategy for remote functionalization iminyl radicals: radical ring-opening-arylation, -vinylation and -alkylation cascades.

[This corrects the article DOI: 10.1039/C9SC02616A.].

Photoinduced decarboxylative azidation of cyclic amino acids.

The direct decarboxylative azidation of cyclic α-amino acids has been achieved via visible light-mediated organo-photoredox catalysis. This synthetic strategy allows the simple preparation of azide-contaning building blocks and has been used in the selective modification of N-terminal proline residues of two di-peptides.