One-pot, direct incorporation of [11C]CO2 into carbamates.
نویسندگان
چکیده
Why beat about the bush? An operationally simple and mild reaction based on the direct fixation of (11)CO(2) with 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) has been developed for the synthesis of (11)C-labeled carbamates at 75 degrees C within 10 minutes in radiochemical yields above 70% (see scheme). This strategy should be immediately useful for the construction of new radiotracers for positron emission tomography and other applications.
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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عنوان ژورنال:
- Angewandte Chemie
دوره 48 19 شماره
صفحات -
تاریخ انتشار 2009