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US 8,076,464 B2Granted
Methods for carbon isotope labeling synthesis of ketones and amines by Suzuki coupling reactions using carbon-isotope monoxide
AssigneeGe Healthcare Limited
InventorsObaidur Rahman, Bengt Langstrom, Tor Kihlberg, Jordi Llop
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Abstract
Methods and reagents for synthesizing carbon-isotope labeled ketones and amines by carbonylation via Suzuki coupling reaction using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled ketones and amines are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
Claims10
A method for labeling synthesis of ketones, comprising:
- (a) providing a high pressure reaction chamber having a liquid inlet and a gas inlet in a bottom surface thereof,
- (b) providing a solution to be labeled comprising a triflate of formula R1-OTf, wherein R1 is linear or cyclic alkyl or substituted alkyl or a heteroaryl group;
- a boronic acid having a formula RB(OH)2, wherein R is linear or cyclic alkyl or substituted alkyl, aryl or substituted aryl;
- and a transitional metal complex,
- (c) introducing a carbon-isotope monoxide enriched gas-mixture into the reaction chamber of the UV reactor assembly via the gas inlet,
- (d) introducing at high pressure said solution mixed with transition metal complex into the reaction chamber via the liquid inlet,
- (e) waiting for a predetermined time while the labeling synthesis occur, and
- (f) removing the labeled ketones from the reaction chamber.
5 more elements
Dependencies are inferred from the claim text.