A New Approach for a 11C-C Bond Formation: Synthesis of 17alpha-(3'-[11C]Prop-1-yn-1-yl)-3-Methoxy-3,17beta-Estradiol


A New Approach for a 11C-C Bond Formation: Synthesis of 17alpha-(3'-[11C]Prop-1-yn-1-yl)-3-Methoxy-3,17beta-Estradiol

Wüst, F.; Zessin, J.; Johannsen, B.

A new approach for a 11C-C bond formation via a Sonogashira-like cross-coupling reaction of terminal alkynes with [11C]methyl iodide was exemplified by the synthesis of 17alpha-(3'-[11C]prop-1-yn-1-yl)-3-methoxy-3,17beta-estradiol. The title compound was obtained in decay-corrected radiochemical yields of 27-47% (n=8) based on [11C]methyl iodide within 21-27 minutes after EOB. In a typical synthesis, 1-2 GBq of 17alpha-(3'-[11C]prop-1-yn-1-yl)-3-methoxy-3,17beta-estradiol was synthesized in radiochemical purity >99%. The specific activity ranged between 10-19 GBq/µmol, and the labeling position was verified by the synthesis of the corresponding 13C-labeled compound.

  • Journal of Labelled Compounds and Radiopharmaceuticals 46 (2003) 333-342

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Publ.-Id: 4520