Approach to Heterospirocycles for Medicinal Chemistry
The gold(I)-catalyzed cycloisomerization of aliphatic 1-bromoalkynes has been applied to the synthesis of heterospirocycles. The reactivity of the C(sp<sup>2</sup>)-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<sub>2</sub>H, NH<sub>2</sub>, OH, and Bpin) were readily obtained. These spirocyclic compounds are valuable building blocks for modern drug discovery projects.
Authors
- Rubén Miguélez
- Pavel K. Mykhailiuk (ORCID: https://orcid.org/0000-0003-1821-9011)
- Pablo Barrio (ORCID: https://orcid.org/0000-0001-7101-4037)
- Carlos Rodríguez‐Arias (ORCID: https://orcid.org/0000-0002-6929-7979)
- Yuliia Holota (ORCID: https://orcid.org/0009-0009-2329-7111)
Institutions
- Universidad de Oviedo (ES)
- Taras Shevchenko National University of Kyiv (UA)
- Enamine (Ukraine) (UA)
Publication Details
- Journal
- Organic Letters
- Published
- 2025-09-05
- DOI
- https://doi.org/10.1021/acs.orglett.5c03125
- Citations
- 4
- Primary Topic
- Catalytic Alkyne Reactions
- Type
- article
- Field-Weighted Citation Impact
- 3.74
Funders
- Agencia Estatal de Investigación