发明名称 PROCESS FOR PRODUCTION OF RADIOACTIVE-FLUORINE-LABELED ORGANIC COMPOUND
摘要 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 R 1 is a straight or branched alkyl chain with 1-10 carbon atoms or an aromatic substituent, R 2 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 R 3 is a protective group) is heated under stirring in an inert organic solvent in a presence of a phase transfer catalyst, 16 F 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.
申请公布号 EP2230229(A4) 申请公布日期 2010.11.24
申请号 EP20080863261 申请日期 2008.12.16
申请人 NIHON MEDI-PHYSICS CO., LTD. 发明人 KUROSAKI, FUMIE;TOYAMA, MASAHITO;HAYASHI, AKIO
分类号 C07C269/06;C07B59/00;C07B61/00;C07C271/24 主分类号 C07C269/06
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