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Paper

Org. Biomol. Chem., 2010, 8, 428 - 432, DOI: 10.1039/b916419g

Direct fixation of [11C]-CO2 by amines: formation of [11C-carbonyl]-methylcarbamates

Alan A. Wilson, Armando Garcia, Sylvain Houle and Neil Vasdev

[11C-Carbonyl]-methylcarbamates can be synthesised directly from [11C]-CO2 and primary or secondary amines in a one-pot, two-step reaction. The use of either diazabicyclo[5.4.0]undec-7-ene (DBU) or 2-tert-butylimino-2-diethylamino-1,3-dimethyl-perhydro-1,3,2-diazaphosphorine (BEMP) enables efficient trapping of [11C]-CO2 in small volumes of DMF as [11C]-carbamate salts. Subsequent reaction with a variety of methylating agents rapidly generates the desired [11C-carbonyl]-methylcarbamates in high radiochemical yields. The usefulness of the method is illustrated by the efficient radiosynthesis of a kappa opioid receptor imaging radiotracer, useful in positron emission tomography (PET).

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