Rapid and efficient synthesis of [11C]ureas via the incorporation of [11C]CO2 into aliphatic and aromatic amines.
نویسندگان
چکیده
A rapid urea radiolabelling methodology has been developed. [(11)C]CO2 was activated by 1,8-diazabicycloundec-7-ene (DBU) in the presence of aliphatic and aromatic amines and reacted with Mitsunobu reagents to produce asymmetric (11)C radiolabelled ureas in high radiochemical yields.
منابع مشابه
From [11C]CO2 to [11C]amides: a rapid one-pot synthesis via the Mitsunobu reaction† †Electronic supplementary information (ESI) available: Experimental details and NMR spectra. See DOI: 10.1039/c7cc01407d
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 rad...
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ورودعنوان ژورنال:
- Chemical communications
دوره 49 74 شماره
صفحات -
تاریخ انتشار 2013