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From [¹¹C]CO₂ to [¹¹C]amides: a rapid one-pot synthesis via the Mitsunobu reaction

Author:
Bongarzone, S., Runser, A., Taddei, C., Dheere, A. K. Haji, Gee, A. D.
Source:
Chemical communications 2017 v.53 no.38 pp. 5334-5337
ISSN:
1364-548X
Subject:
Grignard reagents, amides, carbon dioxide, chemical reactions, melatonin, synthesis
Abstract:
A novel amide synthesis methodology is described using amines, CO₂ and Grignard reagents and Mitsunobu reagents. The method was applied to carbon-11 radiochemistry to label amides using cyclotron-produced [¹¹C]CO₂. The synthetic utility of the one-pot labelling methodology was demonstrated by producing [¹¹C]melatonin. The incorporation of [¹¹C]CO₂ into [¹¹C]melatonin was 36% – determined by radioHPLC 2 min post [¹¹C]CO₂ delivery.
Agid:
6391203