Cross-coupling

During lead optimization, medicinal chemists often need to introduce small C(sp³) fragments—such as methyl, cyclopropyl, difluoromethyl, hydroxymethyl, oxetanyl, and bicyclo[1.1.1]pentyl groups—onto the same molecular scaffold to investigate how changes in substituents affect biological ...

Cross-coupling refers to the connection of two molecular fragments under the action of a metal catalyst to form a new chemical bond. In organic synthesis, these reactions are most commonly used to construct carbon–carbon bonds, and they have also been widely extended to carbon–nitrogen and ...

Haloheterocycles have long occupied an important place in modern organic synthesis not simply because they are “heterocycles bearing halogens,” but because they simultaneously provide two layers of information: the heterocyclic core and an editable site.

In cross-coupling (especially Pd-catalyzed C–N/C–C bond formation), researchers often set multiple goals at once: more challenging substrates (Ar–Cl/heteroaryl chlorides), less metal (low Pd loading), larger scale (scale-up), and tighter control of outcomes (stable impurity profile and ...

C(sp2)- and C(sp)-hybridized coupling reactions are established catalytic approaches. However, multi-step C(sp3)- and C(sp2)-coupling reactions of boronic acids and related derivatives are still limited by ineffective two-electron transmetalation reactions. These conventional protocols exhibit ...