Org. Lett. 2025, 27, 37, 10342–10347
DOI: 10.1021/acs.orglett.5c03125
Rodriguez-Arias C.; Miguelez R.; Holota Y.; Mykhailiuk P.; Barrio P.
The gold(I)-catalyzed cycloisomerization of aliphatic 1-bromoalkynes has been applied to the synthesis of heterospirocycles. The reactivity of the C(sp2)–Br bond in the products allowed for further derivatization of the obtained scaffolds. In this way, spiroheterocycles decorated with a plethora of functional groups (i.e., CO2H, NH2, OH, and Bpin) were readily obtained. These spirocyclic compounds are valuable building blocks for modern drug discovery projects.