Improvements of C–H Radio-Iodination of N-Acylsulfonamides toward Implementation in Clinics

An improved protocol to perform C–H radio-iodination is described. These new conditions allow rapid and clean formation of radio-iodinated N-acylsulfonamides using [125I]NIS and catalytic amounts of palladium acetate and para-toluenesulfonic acid. No pre-functionalized precursors are required and the products are obtained with radiochemical conversions (RCC) of 27–84%.

Mots clés

radiochemistry iodination C–H activation palladium iodine-125

Domaines

Radiochimie

Thomas Cailly : Connectez-vous pour contacter le contributeur

https://hal.science/hal-02400013

Soumis le : lundi 9 décembre 2019-12:38:45

Dernière modification le : jeudi 11 avril 2024-13:08:13

Dates et versions

hal-02400013 , version 1 (09-12-2019)

Identifiants

HAL Id : hal-02400013 , version 1
DOI : 10.1055/s-0037-1611884

Citer

Emmanuelle Dubost, Victor Babin, Florian Benoist, Alexandra Hébert, Gilbert Pigrée, et al.. Improvements of C–H Radio-Iodination of N-Acylsulfonamides toward Implementation in Clinics. Synthesis: Journal of Synthetic Organic Chemistry, 2019, 51 (23), pp.4393-4400. ⟨10.1055/s-0037-1611884⟩. ⟨hal-02400013⟩

Exporter

BibTeX XML-TEI Dublin Core DC Terms EndNote DataCite

Collections

CNRS INSA-ROUEN COMUE-NORMANDIE INC-CNRS UNIROUEN ENSICAEN UNILEHAVRE UNICAEN COBRA INSA-GROUPE CERMN LABOS-XL-CHEM

45 Consultations

0 Téléchargements