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


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.

SUBMITTER: van der Wildt B 

PROVIDER: S-EPMC7454003 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature

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Efficient synthesis of carbon-11 labelled acylsulfonamides using [<sup>11</sup>C]CO carbonylation chemistry.

van der Wildt Berend B   Shen Bin B   Chin Frederick T FT  

Chemical communications (Cambridge, England) 20190301 21


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. ...[more]

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