Efficient synthesis of carbon-11 labelled acylsulfonamides using [11C]CO carbonylation chemistry

Berend van der Wildt; Bin Shen; Frederick T. Chin

doi:10.1039/C8CC09661A

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Efficient synthesis of carbon-11 labelled acylsulfonamides using [¹¹C]CO carbonylation chemistry†

Berend van der Wildt,

^a Bin Shen^a and Frederick T. Chin

*^a

Author affiliations

* Corresponding authors

^a Stanford University, School of Medicine, Department of Radiology, Molecular Imaging Program at Stanford (MIPS), 1201 Welch Road, PS049, Stanford, CA, USA
E-mail: chinf@stanford.edu

Abstract

Herein, a novel method for carbon-11 labeling of acyl sulfonamides by a one-step insertive [¹¹C]CO carbonylative cross-coupling reaction between aryl halides and sulfonamides is presented. Various model compounds as well as drug molecules LY573636 (tasisulam) and ABT-199 were obtained in excellent yields. This method provides a valuable and widely applicable contribution to the continuously expanding radiochemical toolbox for PET research.

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Article information

DOI: https://doi.org/10.1039/C8CC09661A
Article type: Communication
Submitted: 05 Dec 2018
Accepted: 18 Feb 2019
First published: 19 Feb 2019

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Chem. Commun., 2019,55, 3124-3127

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Efficient synthesis of carbon-11 labelled acylsulfonamides using [¹¹C]CO carbonylation chemistry

B. van der Wildt, B. Shen and F. T. Chin, Chem. Commun., 2019, 55, 3124 DOI: 10.1039/C8CC09661A

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