Late-Stage Radical C-H Alkylamination of Tyrosine Compounds and Phenol-Containing Drugs.

Autor: Andrade-Sampedro P; University of the Basque Country (UPV/EHU), Department of Organic Chemistry I, Joxe Mari Korta R&D Center, Avda. Tolosa 72, 20018 Donostia-San Sebastián, Spain., Correa A; University of the Basque Country (UPV/EHU), Department of Organic Chemistry I, Joxe Mari Korta R&D Center, Avda. Tolosa 72, 20018 Donostia-San Sebastián, Spain.
Jazyk: angličtina
Zdroj: Organic letters [Org Lett] 2024 Oct 18; Vol. 26 (41), pp. 8668-8673. Date of Electronic Publication: 2024 Oct 03.
DOI: 10.1021/acs.orglett.4c02678
Abstrakt: 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 3 as catalyst along with triflic acid as Brønsted acid, thereby enabling the predictable appendance of morpholine and related heterocycles at the ortho C-H bond of phenols in a late-stage fashion.
Databáze: MEDLINE