A phosphine-mediated oxygen-atom replacement of non-strained cyclic ethers is reported, enabling rapid assembly of N-, S-, and Se-heterocyclic and carbocyclic molecules. Remarkable functional group compatibility and applications in pharmaceutical synthesis highlight the utility of this strategy in drug discovery.

The synthesis of unprotected C-heteroaryl glycosides is challenging because of the lack of methods to utilize native saccharides as substrates. Now these compounds, capped as redox-active glycosyl sul...

A divergent electrochemical nitrogen atom insertion into saturated carbocycles is reported, enabling selective access to either functionalized quinolines or N-alkylated saturated N heterocycles. This ...

Molecular-editing method trades oxygen for other atoms to diversify fragments on the fly

Researchers from NUS have pioneered a photocatalytic atom-swapping transformation that converts oxetanes into a variety of four-membered saturated cyclic molecules, which are key scaffolds in medicinal chemistry.

Skeletal editing pushed beyond aromatic structures, sparking new opportunities in drug discovery

Three-component, iron-based catalytic transformations offer a promising and sustainable approach to building complex molecules in a single step. This Review highlights advances and ongoing challenges ...

γ-Lactams are privileged five-membered pharmaco-phores in numerous bioactive compounds, but access to these motifs typically rely on cycloaddition/substitution chemistry involving activated substrate...

Catalytic methods to introduce fluorine into the backbone of small-ring heterocycles are challenging due to the problems of strain-induced ring cleavage and defluorination. Now, a copper catalyst medi...