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Synthesis 2019; 51(23): 4393-4400
DOI: 10.1055/s-0037-1611884
DOI: 10.1055/s-0037-1611884
special topic
Improvements of C–H Radio-Iodination of N-Acylsulfonamides toward Implementation in Clinics
The authors are grateful for financial support provided by the Regional Council of Normandy, FEDER, Crunch Network, la Ligue Contre le Cancer, The ARC foundation, the University of Caen, Tremplin Carnot I2C and the French Ministry of Research.Further Information
Publication History
Received: 29 May 2019
Accepted after revision: 18 June 2019
Publication Date:
09 July 2019 (online)
Published as part of the Special Topic Halogenation methods (with a view towards radioimaging applications)
Abstract
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%.
Supporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0037-1611884.
- Supporting Information
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