Approach to Heterospirocycles for Medicinal Chemistry

High Resolution Image Download MS PowerPoint Slide The gold(I)-catalyzed cycloisomerization of aliphatic 1-bromoalkynes has been applied to the synthesis of heterospirocycles. The reactivity of the C(sp 2 )–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., CO 2 H, NH 2, OH, and Bpin) were readily obtained. These spirocyclic compounds are valuable building blocks for modern drug discovery projects.