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Updated: Sep 19, 2025

Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
Preparation of 211At-Labeled (Hetero)aryl Compounds from Triarylsulfonium and Dibenzothiophenium Salts
Clémence Maingueneau1, Romain Eychenne1,2, Jean-Francois Gestin1
1Nantes Université, Inserm, CNRS, Université d'Angers, CRCI2NA, 44000 Nantes, France.
Abstract:
211At-labeled (hetero)aryl compounds were obtained from arylsulfonium salt in high RCY with a short reaction time. Benzothiophenium salts appear to be superior to triarylsulfonium salts with a high efficiency demonstrated on electronically enriched or depleted phenyl rings and an ortho-substituted substrate. As a potential application, a 211At-labeled benzylazide prosthetic group was produced and conjugated to octreotate by SPAAC. This procedure offers an alternative to previous approaches that generally require toxic or unstable precursors and/or catalysts, and/or lead to inseparable products.
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