Process for production of radioactive-fluorine-labeled organic compound
US8269035B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 16, 2008 |
| Grant date | Sep 18, 2012 |
| Priority date | — |
| Expiry date | Dec 16, 2028 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A process for production of a radioactive fluorine-labeled organic compound is provided which can improve the yield of radioactive fluorination. Provided is a process in which a compound represented by the following formula (1):(wherein R1 is a straight or branched alkyl chain with 1-10 carbon atoms or an aromatic substituent, R2 is a straight or branched haloalkylsulfonic acid substituent with 1-10 carbon atoms, a straight or branched alkylsulfonic acid substituent with 1-10 carbon atoms, a fluorosulfonic acid substituent or an aromatic sulfonic acid substituent, and R3 is a protective group) is heated under stirring in an inert organic solvent in a presence of a phase transfer catalyst, 18F ions and potassium ions, so as to effect labeling with a radioactive fluorine, wherein the heating temperature is 40-90° C., and the concentration of the phase transfer catalyst in the inert organic solvent is 70 mmol/L or more. Preferably, the molar ratio of the phase transfer catalyst is 0.7 or more relative to the compound of the formula (1), and the concentration of the compound of the formula (1) in the inert organic solvent is 50 mmol/L or more.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.