From [(11)C]CO(2) to [(11)C]amides: a rapid one-pot synthesis via the Mitsunobu reaction

从[(11)C]CO(2)到[(11)C]酰胺:通过Mitsunobu反应快速一锅合成

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Abstract

A novel amide synthesis methodology is described using amines, CO(2) and Grignard reagents and Mitsunobu reagents. The method was applied to carbon-11 radiochemistry to label amides using cyclotron-produced [(11)C]CO(2). The synthetic utility of the one-pot labelling methodology was demonstrated by producing [(11)C]melatonin. The incorporation of [(11)C]CO(2) into [(11)C]melatonin was 36% - determined by radioHPLC 2 min post [(11)C]CO(2) delivery.

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