Late-Stage Radical C–H Alkylamination of Tyrosine Compounds and Phenol-Containing Drugs
A modular site-selective iron-catalyzed radical amination of a number of phenol-containing biomolecules such as tyrosine-containing peptides, estrogens, and other phenol-based pharmaceuticals has been developed. The method features the use of the cost-efficient combination of FeBr<sub>3</sub> as catalyst along with triflic acid as Brønsted acid, thereby enabling the predictable appendance of morpholine and related heterocycles at the <i>ortho</i> C-H bond of phenols in a late-stage fashion.
Authors
- Paula Andrade‐Sampedro (ORCID: https://orcid.org/0000-0002-6643-1052)
- Arkaitz Correa (ORCID: https://orcid.org/0000-0002-9004-3842)
Institutions
- University of the Basque Country (ES)
Publication Details
- Journal
- Organic Letters
- Published
- 2024-10-03
- DOI
- https://doi.org/10.1021/acs.orglett.4c02678
- Citations
- 7
- Primary Topic
- Radical Photochemical Reactions
- Type
- article
- Field-Weighted Citation Impact
- 1.75
Funders
- Eusko Jaurlaritza
- Euskal Herriko Unibertsitatea
- Ministerio de Ciencia e Innovación
- European Regional Development Fund
- Agencia Estatal de Investigación
- European Social Fund